Alisertib (MLN8237)

Name: Alisertib (MLN8237)
Brand: Selleck Chemicals
SKU: S1133
Rating: 5 (199 reviews)

For research use only. Not for use in humans.

Catalog No.S1133

199 publications

Molecular Weight(MW): 518.92

Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Phase 3.

Selleck's Alisertib (MLN8237) has been cited by 199 publications

Nature, 2019, 574(7777):268-272

PubMed: 31578521 ( click the link to review the publication )

Science, 2019, 364(6447)

PubMed: 31249032 ( click the link to review the publication )

Cancer Cell, 2019, 36(2):179-193

PubMed: 31378681 ( click the link to review the publication )

Cell, 2019, 36(2):179-193

PubMed: 28162770 ( click the link to review the publication )

Cancer Cell, 2019, 35(5):752-766

PubMed: 31085176 ( click the link to review the publication )

Nat Med, 2016, 22(7):744-53

PubMed: 27213815 ( click the link to review the publication )

Cancer Cell, 2014, 26(3):414-427

PubMed: 25175806 ( click the link to review the publication )

Cell Stem Cell, 2012, 11(2):179-94

PubMed: 22862944 ( click the link to review the publication )

Nat Commun, 2019, 10(1):2189

PubMed: 31097698 ( click the link to review the publication )

Nat Commun, 2019, 10(1):3485

PubMed: 31375684 ( click the link to review the publication )

Nat Commun, 2019, 10(1):993

PubMed: 30824690 ( click the link to review the publication )

Nat Commun, 2019, 10(1):5566

PubMed: 31804482 ( click the link to review the publication )

Nat Commun, 2019, 10(1):2208

PubMed: 31101817 ( click the link to review the publication )

Clin Cancer Res, 2019, 25(14):4552-4566

PubMed: 30979745 ( click the link to review the publication )

Clin Cancer Res, 2019, 25(11):3430-3442

PubMed: 30755439 ( click the link to review the publication )

Dev Cell, 2019, 50(3):355-366e6

PubMed: 31303441 ( click the link to review the publication )

Cell Syst, 2019, 9(1):74-92.e8

PubMed: 31302152 ( click the link to review the publication )

Cell Syst, 2019, 8(2):163-167

PubMed: 30797774 ( click the link to review the publication )

Cell Rep, 2019, 26(2):293-301e7

PubMed: 30625311 ( click the link to review the publication )

Oncogene, 2019, 38(1):73-87

PubMed: 30082913 ( click the link to review the publication )

EBioMedicine, 2019, 41:120-133

PubMed: 30799199 ( click the link to review the publication )

Cell Death Dis, 2019, 10(12):881

PubMed: 31754113 ( click the link to review the publication )

Cancers (Basel), 2019, 11(2)

PubMed: 30736342 ( click the link to review the publication )

Cell Death Dis, 2019, 10(8):606

PubMed: 31406104 ( click the link to review the publication )
FASEB J, 2019, 33(4):4866-4882

PubMed: 30596512 ( click the link to review the publication )

Cell Chem Biol, 2019, 10.1016/j.chembiol.2019.06.003

PubMed: 31257184 ( click the link to review the publication )

PLoS Negl Trop Dis, 2019, 13(5):e0007425

PubMed: 31095613 ( click the link to review the publication )

Antiviral Res, 2019, 170:104572

PubMed: 31376425 ( click the link to review the publication )

Toxicol Sci, 2019, 10.1093/toxsci/kfz123

PubMed: 31132080 ( click the link to review the publication )

Sci Rep, 2019, 9(1):2211

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Transl Oncol, 2019, 12(4):683-692

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Target Oncol, 2019, 14(5):563-575

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Oncotarget, 2019, 10(17):1649-1659

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Blood Adv, 2019, 3(21):3214-3227

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Nat Chem Biol, 2018, 14(8):768-777

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Neuro Oncol, 2018, 20(2):203-214

PubMed: 29016820 ( click the link to review the publication )

Curr Biol, 2018, 28(21):3458-3468e5

PubMed: 30415701 ( click the link to review the publication )

Clin Cancer Res, 2018, 24(24):6594-6610

PubMed: 30181387 ( click the link to review the publication )

Elife, 2018, doi: 107554/eLife38111

PubMed: 30070631 ( click the link to review the publication )

Thyroid, 2018, doi: 101089/thy20180183

PubMed: 30226440 ( click the link to review the publication )

Oncogene, 2018, 37(33):4599-4610

PubMed: 29755130 ( click the link to review the publication )

Oncogene, 2018, 37(22):2921-2935

PubMed: 29515234 ( click the link to review the publication )

Oncogene, 2018, 37(4):502-511

PubMed: 28967900 ( click the link to review the publication )

Cell Death Dis, 2018, 9(8):781

PubMed: 30013101 ( click the link to review the publication )

Mol Cancer Ther, 2018, 17(12):2575-2585

PubMed: 30266802 ( click the link to review the publication )

Mol Cancer Ther, 2018, 17(12):2551-2563

PubMed: 30217967 ( click the link to review the publication )

Mol Cell Proteomics, 2018, 17(12):2434-2447

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Mol Pharm, 2018, 15(8):3046-3059

PubMed: 29863884 ( click the link to review the publication )
Int J Mol Sci, 2018, 19(12)

PubMed: 30544932 ( click the link to review the publication )

Apoptosis, 2018, 23(9-10):492-511

PubMed: 30027525 ( click the link to review the publication )

Int J Mol Sci, 2018, 19(12)

PubMed: 30544932 ( click the link to review the publication )

Cell Cycle, 2018, 17(5):652-668

PubMed: 28749250 ( click the link to review the publication )

BMC Cancer, 2018, 18(1):922

PubMed: 30253737 ( click the link to review the publication )

BMC Cancer, 2018, 18(1):922

PubMed: 30253737 ( click the link to review the publication )

J Cancer, 2018, 9(12):2061-2071

PubMed: 29937924 ( click the link to review the publication )

Cancer Med, 2018, 7(11):5589-5603

PubMed: 30221846 ( click the link to review the publication )

Int J Mol Med, 2018, 41(6):3629-3641

PubMed: 29512701 ( click the link to review the publication )

Pediatr Blood Cancer, 2018, 65(8):e27094

PubMed: 29697184 ( click the link to review the publication )

Pediatr Blood Cancer, 2018, 65(8):e27094

PubMed: 29697184 ( click the link to review the publication )

Mol Med Rep, 2018, 18(1):1206-1210

PubMed: 29845253 ( click the link to review the publication )

Anticancer Res, 2018, 38(6):3471-3476

PubMed: 29848699 ( click the link to review the publication )

Oncotarget, 2018, 9(89):35875-35890

PubMed: 30542505 ( click the link to review the publication )

Oncotarget, 2018, 9(89):35875-35890

PubMed: 30542505 ( click the link to review the publication )

Oncotarget, 2018, 9(65):32496-32506

PubMed: 30197758 ( click the link to review the publication )

Sci Rep, 2018, 8(1):14017

PubMed: 30228302 ( click the link to review the publication )

Oncotarget, 2018, 9(16):12769-12780

PubMed: 29560108 ( click the link to review the publication )

SLAS Discov, 2018, 23(8):850-861

PubMed: 29742358 ( click the link to review the publication )

J Neurooncol, 2018, 137(3):481-492

PubMed: 29396807 ( click the link to review the publication )

Oncotarget, 2018, 9(65):32496-32506

PubMed: 30197758 ( click the link to review the publication )

R Soc Open Sci, 2018, 5(12):181303

PubMed: 30662739 ( click the link to review the publication )

Sci Transl Med, 2017, 9(372)

PubMed: 28077684 ( click the link to review the publication )

Mol Cell, 2017, 68(1):210-223e6

PubMed: 28985505 ( click the link to review the publication )
Nat Commun, 2017, 8:14294

PubMed: 28220783 ( click the link to review the publication )

Clin Cancer Res, 2017, 10.1158/1078-0432

PubMed: 28073841 ( click the link to review the publication )

EBioMedicine, 2017, 24:43-55

PubMed: 29030058 ( click the link to review the publication )

Plant Physiol, 2017, 173(1):582-599

PubMed: 27879390 ( click the link to review the publication )

FASEB J, 2017, 32(2):625-638

PubMed: 28970258 ( click the link to review the publication )

Cell Physiol Biochem, 2017, 43(1):94-107

PubMed: 28848145 ( click the link to review the publication )

Mol Cancer Ther, 2017, 16(9):1934-1941

PubMed: 28522591 ( click the link to review the publication )

Mol Cancer Ther, 2017, 16(10):2083-2093

PubMed: 28615297 ( click the link to review the publication )

Mol Cancer Ther, 2017, 16(11):2552-2562

PubMed: 28847989 ( click the link to review the publication )

Eur J Med Chem, 2017, 140:1-19

PubMed: 28918096 ( click the link to review the publication )

Mol Cancer Res, 2017, 15(6):670-682

PubMed: 28235899 ( click the link to review the publication )

Mol Cancer Res, 2017, 15(8):984-997

PubMed: 28442587 ( click the link to review the publication )

Cell Discov, 2017, 3:16049

PubMed: 28101375 ( click the link to review the publication )

Sci Rep, 2017, 7:45514

PubMed: 28358124 ( click the link to review the publication )

J Biol Chem, 2017, 292(5):1910-1924

PubMed: 28028179 ( click the link to review the publication )

Am J Transl Res, 2017, 9(10):4652-4672

PubMed: 29118925 ( click the link to review the publication )

Am J Transl Res, 2017, 9(3):845-873

PubMed: 28386317 ( click the link to review the publication )

BMC Cell Biol, 2017, 18(1):33

PubMed: 29141582 ( click the link to review the publication )

Curr Cancer Drug Targets, 2017, 17(4):386-401

PubMed: 27396604 ( click the link to review the publication )

Oncotarget, 2017, 8(10):16669-16689

PubMed: 28035071 ( click the link to review the publication )

Oncotarget, 2017, 8(31):50376-50392

PubMed: 28881569 ( click the link to review the publication )

Oncotarget, 2017, 8(19):32117-32133

PubMed: 28389630 ( click the link to review the publication )

Sci Rep, 2017, 7(1):17978

PubMed: 29269934 ( click the link to review the publication )

Sci Rep, 2017, 7:45514

PubMed: 28358124 ( click the link to review the publication )
Oncotarget, 2017, 8(68):112313-112329

PubMed: 29348827 ( click the link to review the publication )

Oncotarget, 2017, 8(12):19738-19759

PubMed: 28160569 ( click the link to review the publication )

Oncotarget, 2017, 8(41):69691-69708

PubMed: 29050234 ( click the link to review the publication )

Oncotarget, 2017, 8(63):107076-107088

PubMed: 29291012 ( click the link to review the publication )

Oncotarget, 2017, 8(59):100326-100338

PubMed: 29245981 ( click the link to review the publication )

Oncotarget, 2017, 8(70):114474-114480

PubMed: 29383095 ( click the link to review the publication )

Oncotarget, 2017, 8(12):19478-19490

PubMed: 28061448 ( click the link to review the publication )

Oncotarget, 2017, 8(54):92926-92942

PubMed: 29190967 ( click the link to review the publication )

Pharmaceuticals (Basel), 2017, 10(3)

PubMed: 29036881 ( click the link to review the publication )

Oncotarget, 2017, 8(31):50376-50392

PubMed: 28881569 ( click the link to review the publication )

Oncotarget, 2017, 8(34):57047-57057

PubMed: 28915653 ( click the link to review the publication )

Nat Commun, 2016, 7:10180

PubMed: 26782714 ( click the link to review the publication )

Nat Commun, 2016, 7:11389

PubMed: 27091106 ( click the link to review the publication )

Nat Commun, 2016, 7:12674

PubMed: 27624869 ( click the link to review the publication )

J Med Chem, 2016, 59(15):7188-211

PubMed: 27391133 ( click the link to review the publication )

Arch Toxicol, 2016, 291(10):4939-54

PubMed: 26404763 ( click the link to review the publication )

Cell Death Dis, 2016, 7:e2135

PubMed: 26962685 ( click the link to review the publication )

ACS Chem Biol, 2016, 11(12):3400-3411

PubMed: 27768280 ( click the link to review the publication )

Sci Rep, 2016, 6:19567

PubMed: 26777522 ( click the link to review the publication )

Cancer Biol Ther, 2016, 17(5):566-76

PubMed: 27082306 ( click the link to review the publication )

Cell Cycle, 2016, 15(3):413-24

PubMed: 26713495 ( click the link to review the publication )

Onco Targets Ther, 2016, 9:3473-84

PubMed: 27366084 ( click the link to review the publication )

Biochem Biophys Res Commun, 2016, 475(3):251-6

PubMed: 27233613 ( click the link to review the publication )

Exp Hematol, 2016, 44(4):247-56

PubMed: 26724640 ( click the link to review the publication )
Mol Med Rep, 2016, 14(1):394-8

PubMed: 27177156 ( click the link to review the publication )

Biol Bull, 2016, 231(1):61-72

PubMed: 27638695 ( click the link to review the publication )

Oncotarget, 2016, 7(22):33152-64

PubMed: 27121204 ( click the link to review the publication )

Oncotarget, 2016, 7(51):84718-84735

PubMed: 27713168 ( click the link to review the publication )

Oncotarget, 2016, 7(51):84675-84687

PubMed: 27835869 ( click the link to review the publication )

Nat Cell Biol, 2015, 17(2):113-22

PubMed: ( click the link to review the publication )

Nat Cell Biol, 2015, 17(2):113-22

PubMed: 25599390 ( click the link to review the publication )

Nat Commun, 2015, 6:8388

PubMed: 26399523 ( click the link to review the publication )

Mol Cancer, 2015, 14(1):83

PubMed: 25889801 ( click the link to review the publication )

J Invest Dermatol, 2015, 135(9):2292-2300

PubMed: 25848977 ( click the link to review the publication )

J Cell Sci, 2015, 128(2):364-72

PubMed: 25395580 ( click the link to review the publication )

J Cell Sci, 2015, 128(3):516-26

PubMed: 25501815 ( click the link to review the publication )

J Cell Sci, 2015, 128(20):3769-80

PubMed: 26349807 ( click the link to review the publication )

J Cell Sci, 2015, 128(3):527-40

PubMed: 25501809 ( click the link to review the publication )

J Cell Sci, 2015, 128(2):364-72

PubMed: ( click the link to review the publication )

Int J Mol Sci, 2015, 17(1)

PubMed: 26729093 ( click the link to review the publication )

Breast Cancer Res Tr, 2015, 149(3):715-26

PubMed: 25667100 ( click the link to review the publication )

Cell Cycle, 2015, 14(24):3908-19

PubMed: 26697841 ( click the link to review the publication )

Drug Des Devel Ther, 2015, 9:1555-84

PubMed: 25792811 ( click the link to review the publication )

Drug Des Devel Ther, 2015, 9:575-601

PubMed: 25632225 ( click the link to review the publication )

BMC Res Notes, 2015, 8:484

PubMed: 26415506 ( click the link to review the publication )

Genes Cancer, 2015, 6(5-6):184-213

PubMed: 26124919 ( click the link to review the publication )

Oncotarget, 2015, 6(34):35247-62

PubMed: 26497213 ( click the link to review the publication )

Clin Cancer Res, 2014, 34(5):2269-74

PubMed: 24778030 ( click the link to review the publication )
Oncogene, 2014, 33(42):4985-96

PubMed: 24166501 ( click the link to review the publication )

Oncogene, 2014, 33(27):3550-60

PubMed: 23955083 ( click the link to review the publication )

Cell Death Dis, 2014, 5:e1253

PubMed: 24853431 ( click the link to review the publication )

Cell Death Dis, 2014, 5:e1177

PubMed: 24743732 ( click the link to review the publication )

Cell Death Dis, 2014, 6:e1595

PubMed: 25590805 ( click the link to review the publication )

Endocr Relat Cancer, 2014, 21(5):797-811

PubMed: 25074669 ( click the link to review the publication )

Mol Oncol, 2014, 8(8):1419-28

PubMed: 24953013 ( click the link to review the publication )

Mol Cancer Res, 2014, 12(3):433-9

PubMed: 24336958 ( click the link to review the publication )

Biochim Biophys Acta, 2014, 1843(11):2719-2729

PubMed: 25090971 ( click the link to review the publication )

J Transl Med, 2014, 12(1):200

PubMed: 25082261 ( click the link to review the publication )

Mol Carcinog, 2014, 10.1002/mc.22223

PubMed: 25284017 ( click the link to review the publication )

Cell Cycle, 2014, 13(14):2248-61

PubMed: 24875404 ( click the link to review the publication )

FEBS Lett, 2014, 588(14):2198-205

PubMed: 24857377 ( click the link to review the publication )

Chembiochem, 2014, 15(3):443-50

PubMed: 24403173 ( click the link to review the publication )

PLoS One, 2014, 9(12):e113989

PubMed: 25436453 ( click the link to review the publication )

PLoS One, 2014, 9(3):e92402

PubMed: 24642638 ( click the link to review the publication )

PLoS One, 2014, 9(12):e116048

PubMed: 25545367 ( click the link to review the publication )

PLoS One, 2014, 9(7):e101222

PubMed: 24983972 ( click the link to review the publication )

PLoS One, 2014, 9(9):e108758

PubMed: 25268132 ( click the link to review the publication )

PLoS One, 2014, 9(7):e102741

PubMed: 25048812 ( click the link to review the publication )

PLoS One, 2014,

PubMed: ( click the link to review the publication )

Biochem Biophys Res Commun, 2014, 452(3):845-51

PubMed: 25218503 ( click the link to review the publication )

Neurosci Lett, 2014, 583:199-204

PubMed: 25263789 ( click the link to review the publication )

J Pediatr Surg, 2014, 49(1):159-65

PubMed: 24439602 ( click the link to review the publication )
Oncotarget, 2014, 5(10):2947-61

PubMed: 24930769 ( click the link to review the publication )

Oncotarget, 2014, 5(10):2947-61

PubMed: 24930769 ( click the link to review the publication )

Oncotarget, 2014, 5(15):6229-42

PubMed: 25153724 ( click the link to review the publication )

Oncotarget, 2014, 5(12):4071-86

PubMed: 24901229 ( click the link to review the publication )

Nat Commun, 2013, 4:2656

PubMed: 24141283 ( click the link to review the publication )

EMBO Mol Med, 2013, 5(1):149-66

PubMed: 23180582 ( click the link to review the publication )

Leukemia, 2013, 27(3):560-8

PubMed: 22940834 ( click the link to review the publication )

Cancer Res, 2013, 73(20):6310-22

PubMed: 24067506 ( click the link to review the publication )

EMBO Rep, 2013, 14(9):829-36

PubMed: 23887685 ( click the link to review the publication )

Int J Cancer, 2013, 135(3):751-62

PubMed: 24382688 ( click the link to review the publication )

Oral Oncol, 2013, 49(6):551-9

PubMed: 23481312 ( click the link to review the publication )

ACS Chem Biol, 2013, 8(7):1451-9

PubMed: 23597309 ( click the link to review the publication )

J Cell Sci, 2013, 126(Pt 6):1355-65

PubMed: 23345402 ( click the link to review the publication )

J Cell Sci, 2013, 126(Pt 9):2102-13

PubMed: 23532825 ( click the link to review the publication )

Biochim Biophys Acta, 2013, 1833(10):2220-32

PubMed: 23707954 ( click the link to review the publication )

J Biol Chem, 2013, 289(1):74-88

PubMed: 24273164 ( click the link to review the publication )

Cancer Biol Ther, 2013, 14(5):436-49

PubMed: 23377828 ( click the link to review the publication )

PLoS One, 2013, 8(5):e64306

PubMed: 23717592 ( click the link to review the publication )

PLoS One, 2013, 8(9):e73548

PubMed: 24019927 ( click the link to review the publication )

Oncotarget, 2013, 4(1):80-93

PubMed: 23328114 ( click the link to review the publication )

J Biol Chem, 2012, 287(33):27670-81

PubMed: 22753416 ( click the link to review the publication )

Breast Cancer Res Tr, 2012, 135(2):433-44

PubMed: 22825030 ( click the link to review the publication )

Cell Cycle, 2012, 11(2):296-309

PubMed: 22214762 ( click the link to review the publication )

Cell Cycle, 2012, 11(13):2567-77

PubMed: 22722494 ( click the link to review the publication )
PLoS One, 2012, 7(2):e30734

PubMed: 22359551 ( click the link to review the publication )

EMBO J, 2011, 30(5):906-19

PubMed: 21297582 ( click the link to review the publication )

Mol Cancer, 2011, 10:131

PubMed: 22011530 ( click the link to review the publication )

J Cell Biol, 2010, 191(7):1315-32

PubMed: 21187329 ( click the link to review the publication )

EMBO Rep, 2010, 11(12):977-84

PubMed: 21072059 ( click the link to review the publication )

ACS Chem Biol, 2010, 5(6):563-76

PubMed: 20426425 ( click the link to review the publication )

Expert Opin Emerg Dr, 2010, 15(4):615-34

PubMed: 20690888 ( click the link to review the publication )

Purity & Quality Control

Choose Selective Aurora Kinase Inhibitors

Biological Activity

Description

Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Phase 3.

Features

First orally available inhibitor of Aurora A.

Targets

Aurora A ^[1]
(Cell-free assay)

1.2 nM

In vitro

MLN8237 shows >200-fold higher selectivity for Aurora A than the structurally related Aurora B with an IC50 of 396.5 nM, and does not have any significant activity against 205 other kinases. ^[1] MLN8237 (0.5 μM) treatment inhibits the phosphorylation of Aurora A in MM1.S and OPM1 cells, without affecting the Aurora B mediated histone H3 phosphorylation. MLN8237 significantly inhibits cell proliferation in multiple myeloma (MM) cell lines with IC50 values of 0.003-1.71 μM. MLN8237 displays more potent anti-proliferation activity against primary MM cells and MM cell lines in the presence of BM stroma cells, as well as IL-6 and IGF-1 than against MM cells alone. MLN8237 (0.5 μM) induces 2- to 6-fold increase in G2/M phase in primary MM cells and cell lines, as well as significant apoptosis and senescence, involving the up-regulation of p53, p21 and p27, as well as PARP, caspase 3, and caspase 9 cleavage. In addition, MLN8237 shows strong synergistic anti-MM effect with dexamethasone, as well as additive effect with doxorubicin and bortezomib. ^[2] MLN8237 (0.5 μM) treatment causes the inhibition of colony formation of FLO-1, OE19, and OE33 esophageal adenocarinoma cell lines, and induces a significant increase in the percentage of polyploid cells, and subsequently an increase in the percentage of cells in the sub-G1 phase, which can be further enhanced in combination with cisplatin (2.5 μM), involving the higher induction of TAp73β, PUMA, NOXA, cleaved caspase-3, and cleaved PARP as compared with a single-agent treatment. ^[3]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
HCT116	MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M4X0e\|AvPSEQvF2=	NVruW5NnPzJiaB?=	MXfEUXNQ	NW\PbZZLUUN3ME2wMlA1KM7:TR?=	MkiyNlYyOzZ4OES=
LS174T	NXfWVoYzT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NV74d455OC53IN88US=>	NXvuOoRMPzJiaB?=	NGL2UFFFVVOR	NXPjUXFvUUN3ME2wMlA2KM7:TR?=	M{PrWVI3OTN4Nki0
T84	MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MkXyNE42KM7:TR?=	M4m4S\|czKGh?	MnLwSG1UVw>?	NVrxSlA{UUN3ME2wMlA6KM7:TR?=	M{m5UVI3OTN4Nki0
LS180	NV7qOHl7T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M2nMeFAvPSEQvF2=	NH:1c5M4OiCq	MXHEUXNQ	NYXDb2s3UUN3ME2xJO69VQ>?	NGn4eogzPjF\|Nk[4OC=>
SW948	NUm2dZc4T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M{W5NlAvPSEQvF2=	M{nINlczKGh?	NYDvbJhxTE2VTx?=	MkW1TWM2OD1zIN88US=>	Mo\BNlYyOzZ4OES=
HCT15	MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	Mk[1NE42KM7:TR?=	NIHWS5g4OiCq	NWWxVG5yTE2VTx?=	MlzkTWM2ODxyLkSg{txO	M4HNSFI3OTN4Nki0
DLD-1	MlH5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M1;qbFAvPSEQvF2=	NWXFXZB2PzJiaB?=	M1rQO2ROW09?	M1XUb2lEPTB:MD64JO69VQ>?	NFThW4szPjF\|Nk[4OC=>
MIP-101	Mn\sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M1PH[lAvPSEQvF2=	NWqzXFRkPzJiaB?=	NUH1NZd2TE2VTx?=	MofxTWM2OD1zIN88US=>	NGLwbIEzPjF\|Nk[4OC=>
SNU1544	MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MofVNE42KM7:TR?=	MmG4O\|IhcA>?	M4XNeGROW09?	MkW4TWM2OD1zIN88US=>	M4j0PVI3OTN4Nki0
OCI-Ly10	NFHsWmVEgXSxdH;4bYMhSXO\|YYm=		NITVZo84OiCq	MWXEUXNQ	MXHJR\|UxRTBwMEW4JO69VQ>?	NXrBe212OjV6N{izN\|E>
SU-DHL2	NFLJN4REgXSxdH;4bYMhSXO\|YYm=		MmHVO\|IhcA>?	M{HIbGROW09?	NY\FbZBrUUN3ME2wMlAyKM7:TR?=	NYfIT5VXOjV6N{izN\|E>
OCI-LY7	MVTDfZRwfG:6aXOgRZN{[Xl?		MWq3NkBp	NVnvTo9sTE2VTx?=	NVLGWHF3UUN3ME2wMlA5OSEQvF2=	MlWwNlU5Pzh\|M{G=
SU-DHL6	NX\LOGNES3m2b4TvfIlkKEG\|c3H5		Ml7jO\|IhcA>?	MW\EUXNQ	MVXJR\|UxRTBwNEiyJO69VQ>?	MW[yOVg4QDN\|MR?=
Jeko-1	NUXuVXFiS3m2b4TvfIlkKEG\|c3H5		NXHxO2lqPzJiaB?=	Mn3NSG1UVw>?	MmXYTWM2OD1yLkCyPUDPxE1?	NEfRb3AzPTh5OEOzNS=>
JVM-2	M1TINmN6fG:2b4jpZ{BCe3OjeR?=		MnK0O\|IhcA>?	M{HIPGROW09?	NInQTVNKSzVyPUCuNFEh\|ryP	NInhcXAzPTh5OEOzNS=>
Rec-1	NHzGd\|lEgXSxdH;4bYMhSXO\|YYm=		MU[3NkBp	M3rUV2ROW09?	NH;YWXZKSzVyPUCuNFg4KM7:TR?=	M362T\|I2QDd6M{Ox
Z-138	MlSxR5l1d3SxeHnjJGF{e2G7		NVHLeZc2PzJiaB?=	MknySG1UVw>?	NWHRT257UUN3ME2wMlAyOyEQvF2=	M1e4dFI2QDd6M{Ox
H9	MonSR5l1d3SxeHnjJGF{e2G7		NGr5Ro04OiCq	M17JcmROW09?	MUDJR\|UxRTBwNjFOwG0>	MYmyOVg4QDN\|MR?=
HH	MYPDfZRwfG:6aXOgRZN{[Xl?		NVLjW3VDPzJiaB?=	NYHnOYhFTE2VTx?=	MXTJR\|UxRTBwNzFOwG0>	Ml;aNlU5Pzh\|M{G=
DND41	NE\NXopEgXSxdH;4bYMhSXO\|YYm=		NFG4b2I4OiCq	NG\EPFNFVVOR	M4HueWlEPTB;MD6xJO69VQ>?	NEXtVpozPTh5OEOzNS=>
CCL119	M{f6R2N6fG:2b4jpZ{BCe3OjeR?=		M1jERlczKGh?	MUnEUXNQ	NY\zV\|Z5UUN3ME2wMlA3OiEQvF2=	NVXNcVJ7OjV6N{izN\|E>
J.Cam 1.6	NF\qSVNEgXSxdH;4bYMhSXO\|YYm=		NVn1VIlUPzJiaB?=	M{D5NmROW09?	MmDhTWM2OD1yLkGwOUDPxE1?	Mn;1NlU5Pzh\|M{G=
Sup-T1	MlTiR5l1d3SxeHnjJGF{e2G7		MYi3NkBp	NYHH[2FzTE2VTx?=	M3jsS2lEPTB;Mj6xOFIh\|ryP	M4XDdFI2QDd6M{Ox
Tib 152	NWG0S45LS3m2b4TvfIlkKEG\|c3H5		NHHpdlg4OiCq	NILVdJVFVVOR	MWLJR\|UxRTBwODFOwG0>	NHHjOpMzPTh5OEOzNS=>
MCF7	M{LSbGZ2dmO2aX;uJGF{e2G7	NFPFXHk2KM7:TR?=	MoTGNlQhcA>?	MYjEUXNQ	M1TTO2lv\HWlZYOgS\|IwVSCjcoLld5Q>	NEXCWVEzPTh\|NESwNS=>
MDA-MB-231	NHvPS3FHfW6ldHnvckBCe3OjeR?=	MXq1JO69VQ>?	Moe1NlQhcA>?	MVrEUXNQ	M3Pt[2lv\HWlZYOgS\|MwVSCjcoLld5Q>	Mm\oNlU5OzR2MEG=
MCF7	MlO2SpVv[3Srb36gRZN{[Xl?	NUnwWYUxPSEQvF2=	MnPQNlQhcA>?	MUHEUXNQ	MXLE[YNz\WG\|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiQ1TLNU9ETEN{	Mlz0NlU5OzR2MEG=
MCF7	NV30fmJuTnWwY4Tpc44hSXO\|YYm=	MYS1JO69VQ>?	M12yelI1KGh?	NXr2b5JsTE2VTx?=	NIHvSotF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOg>?	NHO4TG4zPTh\|NESwNS=>
MCF7	NV;HTYNzTnWwY4Tpc44hSXO\|YYm=	M4rIOlUh\|ryP	M37GW\|I1KGh?	MYXEUXNQ	NHLlc4hF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gZ5lkdGmwIFKx	M1:5OlI2QDN2NECx
MCF7	M4mydmZ2dmO2aX;uJGF{e2G7	MoXXOUDPxE1?	NXi3TIh3OjRiaB?=	Mm\QSG1UVw>?	MkO2TY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIICyNUBY[WZzL1PpdFE>	NFfsU4EzPTh\|NESwNS=>
MCF7	M{m0b2Z2dmO2aX;uJGF{e2G7	NGj3R5k2KM7:TR?=	M3K5TVI1KGh?	MljBSG1UVw>?	M4LGWGlv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDwNlchU2myMR?=	MXGyOVg{PDRyMR?=
MDA-MB-231	MkO4SpVv[3Srb36gRZN{[Xl?	M1rWRVUh\|ryP	M2TDfFI1KGh?	Mny3SG1UVw>?	NIjWb5ZF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOS:FRFOy	MoDTNlU5OzR2MEG=
MDA-MB-231	NEfPfVJHfW6ldHnvckBCe3OjeR?=	NWjGemp2OSEQvF2=	NVLlOFFOOjRiaB?=	MYPEUXNQ	MXPJcoNz\WG\|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiQ1TLNi=>	MkfpNlU5OzR2MEG=
MDA-MB-231	NYTwSmNvTnWwY4Tpc44hSXO\|YYm=	NGjXRZo2KM7:TR?=	NInQW5czPCCq	NEjpXZpFVVOR	NI\uTopF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gZ5lkdGmwIFKx	NWrsU4tYOjV6M{S0NFE>
MDA-MB-231	NUfQV2M4TnWwY4Tpc44hSXO\|YYm=	NVS5foNvPSEQvF2=	NXnlcHpuOjRiaB?=	M2riW2ROW09?	NXzDdpJZUW6lcnXhd4V{KHSqZTDlfJBz\XO\|aX;uJIxmfmWuIH;mJJAzOSCZYX[xM2NqeDF?	MlmwNlU5OzR2MEG=
MDA-MB-231	MXPGeY5kfGmxbjDBd5NigQ>?	NH\HR282KM7:TR?=	M2\pelI1KGh?	NY\DPJlKTE2VTx?=	NV7BV2UxUW6lcnXhd4V{KHSqZTDlfJBz\XO\|aX;uJIxmfmWuIH;mJJAzPyCNaYCx	MXeyOVg{PDRyMR?=
MDA-MB-231	MoPZSpVv[3Srb36gRZN{[Xl?	NHPQWFc2KM7:TR?=	MonhNlQhcA>?	MVLEUXNQ	NXG0VXM2UW6lcnXhd4V{KHSqZTDlfJBz\XO\|aX;uJIxmfmWuIH;mJJA2Ow>?	NF\5dlQzPTh\|NESwNS=>
MCF7	NYjUZ2RVSXCxcITvd4l{KEG\|c3H5	NES3NHg2KM7:TR?=	M1X2[FI1KGh?	MYrEUXNQ	NHqxWnhKdmS3Y3XzJIFxd3C2b4TpZ{Bl\WG2aB?=	M1jtS\|I2QDN2NECx
MDA-MB-231	NX3ub\|ZESXCxcITvd4l{KEG\|c3H5	NFr5eWI2KM7:TR?=	MXiyOEBp	MkTYSG1UVw>?	M1j0cmlv\HWlZYOgZZBweHSxdHnjJIRm[XSq	MmPvNlU5OzR2MEG=
MCF7	M1jRXmZ2dmO2aX;uJGF{e2G7	M2jUSFEh\|ryP	MUK3NkBp	MYXEUXNQ	MUTJcoR2[2W\|IHH1eI9xcGGpaXOg[IVifGh?	NELUbpUzPTh\|NESwNS=>
MDA-MB-231	NYTL[W9ITnWwY4Tpc44hSXO\|YYm=	MYSxJO69VQ>?	NUP4flRiPzJiaB?=	M2\Re2ROW09?	NELmPGRKdmS3Y3XzJIF2fG:yaHHnbYMh\GWjdHi=	MXGyOVg{PDRyMR?=
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MG-63	NVrkWlhRT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	Mn;SOVAh\|ryP	M4KzTFI1KGh?	NGHpUFZFVVOR	MnjETWM2OD17LkWg{txO	Mn;xNlU4QTJ6MUG=
U-2 OS	MnTHRZBweHSxc3nzJGF{e2G7	NYKyXW4{PSEQvF2=	MmjVNlQhcA>?	NVnkfWpjTE2VTx?=	MkC0TY5lfWOnczDhdI9xfG:2aXOgZ4VtdCCmZXH0bC=>	NWX1eIVHOjV5OUK4NVE>
MG-63	NGfkOHhCeG:ydH;zbZMhSXO\|YYm=	MkPMOUDPxE1?	NVnTWIVGOjRiaB?=	NH;PWHJFVVOR	MoroTY5lfWOnczDhdI9xfG:2aXOgZ4VtdCCmZXH0bC=>	MkS0NlU4QTJ6MUG=
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MG-63	NGnWUVRHfW6ldHnvckBCe3OjeR?=	NGrNU4Q2KM7:TR?=	MWqyOEBp	NEW0enJFVVOR	M3XPWHBzd22xdHXzJIF2fG:yaHHnbYMh[2WubDDk[YF1cA>?	NGm0SIUzPTd7MkixNS=>
PANC-1	M3ricmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MoiwOVAh\|ryP	MlrwNlQhcA>?	NGHqSGNFVVOR	NITHS2dKSzVyPUeuNUDPxE1?	MUeyOVY{OjJ{NR?=
BxPC-3	MmjCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M{XzcVUxKM7:TR?=	Ml\xNlQhcA>?	MoXDSG1UVw>?	M2X1dWlEPTB;Nj64JO69VQ>?	M376[lI2PjN{MkK1
PANC-1	MmCzSpVv[3Srb36gRZN{[Xl?	MV21JO69VQ>?	M1W2elI1KGh?	NFjadJRFVVOR	M3fZVGlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4SgbY4hTzJxTTDwbIF{\Q>?	MWqyOVY{OjJ{NR?=
BxPC-3	MU\GeY5kfGmxbjDBd5NigQ>?	MnPhOUDPxE1?	MV:yOEBp	NHyxNnhFVVOR	MV;JcoR2[2W\|IHPlcIwh[3mlbHWgZZJz\XO2IHnuJGczN01icHjhd4U>	NUnhV2pnOjV4M{KyNlU>
PANC-1	NF;UdVlHfW6ldHnvckBCe3OjeR?=	NFraRpg2KM7:TR?=	NGHWbZYzPCCq	MV\EUXNQ	MVXJcoR2[2W\|IHH1eI9xcGGpaXOgZ4VtdCCmZXH0bC=>	NFnCN44zPTZ\|MkKyOS=>
BxPC-3	NUHEe3RiTnWwY4Tpc44hSXO\|YYm=	MV21JO69VQ>?	M{G3OlI1KGh?	NFntdHhFVVOR	M1[wPWlv\HWlZYOgZZV1d3CqYXfpZ{Bk\WyuIHTlZZRp	M2rOZlI2PjN{MkK1
SKOV3	Mn35S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MYOxNFAh\|ryP	M{HVbFI1KGh?	Mn\mSG1UVw>?	NXvNVmU5UUN3ME2yNE41QCEQvF2=	Ml21NlU3OjR5NUC=
OVCAR4	M4qwb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NVHqeIdjOTByIN88US=>	M4W3elI1KGh?	NEXaRZpFVVOR	MYLJR\|UxRTJ{LkGzJO69VQ>?	NILSZokzPTZ{NEe1NC=>
SKOV3	M3vhXGZ2dmO2aX;uJGF{e2G7	MVW1JO69VQ>?	NELWXII4OiCq	M2rKRmROW09?	MkPaTY5lfWOnczDHNk9OKGG{cnXzeC=>	Ml7SNlU3OjR5NUC=
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OVCAR4	NWexfpg2SXCxcITvd4l{KEG\|c3H5	MlzXOUDPxE1?	NW\nW5J4OjRiaB?=	M1P5XmROW09?	MVXJcoR2[2W\|IHHwc5B1d3Orcx?=	NF\CRlkzPTZ{NEe1NC=>
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NCI-N78	NVHSdGpTT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NGXkWWMzPSEQvF2=	M3rxV\|I1KGh?	MWDEUXNQ	NH\oZ\|VKSzVyPUK2MlM{KM7:TR?=	NE\6W48zPTZyOUmyNy=>
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NCI-N78	MYXBdI9xfG:\|aYOgRZN{[Xl?	M{nPSFUh\|ryP	NWLlfHp2OjRiaB?=	MnvhSG1UVw>?	NVSzVYx3UW6mdXPld{BieG:ydH;zbZM>	NHm2c3YzPTZyOUmyNy=>
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NCI-N78	NHP2elJHfW6ldHnvckBCe3OjeR?=	MmS0OUDPxE1?	NGe1O4UzPCCq	MX3EUXNQ	MonyTY5lfWOnczD0bIUh[XW2b4DoZYd6	NXLLR2JPOjV4MEm5NlM>
HSC-3	MkjsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M3fheVEh\|ryP	M3XSfFQ5KGh?		Mo\FTWM2OD1yLkW0JO69VQ>?	NELMSWMzPTN4NkG0Ny=>
GB30	MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NHvlSYQyKM7:TR?=	NXLme5VUPyCm	M2PTeGROW09?	NWPxVZhVUUN3ME2wMlAyOSEQvF2=	NWXLTIlzOjVzME[0Nlg>
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GB169	M3XO[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NWfRXW9iOSEQvF2=	NWDZUoVPPyCm	NWHzZo1CTE2VTx?=	MUPJR\|UxRTBwMEOyJO69VQ>?	NHGzWnAzPTFyNkSyPC=>
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RT4	M2rP[WZ2dmO2aX;uJGF{e2G7	MnrPNUDPxE1?	MWq0PEBp	MkTFSG1UVw>?	MYTJcoR2[2W\|IHPlcIwh[3mlbHWgZZJz\XO2	M2PQNFI{PDB\|NkOz
UM-UC-3	MVzGeY5kfGmxbjDBd5NigQ>?	MlmwNUDPxE1?	MnrLOFghcA>?	MUTEUXNQ	NVLLbVFWUW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=>	NH;sZmgzOzRyM{[zNy=>
T24	NX7JW4J6SXCxcITvd4l{KEG\|c3H5	MmrzN{4yPiEQvF2=	NFf3O5c6PiCq	MX3EUXNQ	NXXuVWpGUUN3ME2wMlA{ODZizszN	M{jEUlI{PDB\|NkOz
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UM-UC-3	Ml\qRZBweHSxc3nzJGF{e2G7	NEjHSGM{NjF4IN88US=>	NVHJPYxDQTZiaB?=	NWPIb2FDTE2VTx?=	NIPoeZBKSzVyPUCuNFQ1QSEQvF2=	NVjLVWt4OjN2MEO2N\|M>
OVCAR-5	Mmi4SpVv[3Srb36gRZN{[Xl?	M2PtTlUxKG6P			M1;ifWlvcGmkaYTzJINmdGxibXnndoF1cW:w	NID0VHQzOzN\|NEOyOy=>
SKOV3ip2	M3fHOWZ2dmO2aX;uJGF{e2G7	MnLDOVAhdk1?			NEPnUG1KdmirYnn0d{Bk\WyuIH3p[5JifGmxbh?=	NIHZT4wzOzN\|NEOyOy=>
S462	NGHmZ49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MmHlNVAxKM7:TR?=	M2fsPVczKGh?	NF:0TZhFVVOR	MknLRZR1\W63YYTld{Bk\WyuIHfyc5d1cA>?	NFfHUGEzOzN{OEGxOC=>
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2885	NYiwSpZRT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NGPtfY8yODBizszN	NXXR[I1vPzJiaB?=	M{jIdmROW09?	NFXwfIdCfHSnboXheIV{KGOnbHyg[5Jwf3Sq	MWGyN\|MzQDFzNB?=
CRL-2396	NV7h[3I3T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	Ml7kNVAxKM7:TR?=		NXW0Zml{f2G2ZYK=	M3XmNmlEPTB;MD6wPVIh\|ryP	NXfGWpY2OjNzNUO1NlQ>
TIB-48	Mn7GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NHraSFUyODBizszN		MoPwe4F1\XJ?	MXTJR\|UxRTBwMEi4JO69VQ>?	MmfrNlMyPTN3MkS=
CRL-2396	MorBR5l1d3SxeHnjJGF{e2G7	NV7xd\|dIOSEQvF2=	NEfGd3Q1QCCq	NF\uU3N4[XSnch?=	NWq2ZZRzUW6mdXPld{BieG:ydH;zbZM>	NG\XdXQzOzF3M{WyOC=>
TIB-48	MUnDfZRwfG:6aXOgRZN{[Xl?	NH3xbnMyKM7:TR?=	M4PkWlQ5KGh?	M4DMc5difGW{	M{TuXmlv\HWlZYOgZZBweHSxc3nz	M{Lvc\|I{OTV\|NUK0
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FLO-1	M165bGN6fG:2b4jpZ{BCe3OjeR?=	MWGwMlUh\|ryP	MnXRNlQhcA>?	MWrEUXNQ	MmHHSIVkemWjc3XzJINmdGxic4Xyeol3[Wx?	MXSyNlk4OjZzMR?=
OE33	MWrDfZRwfG:6aXOgRZN{[Xl?	NIP4XXYxNjVizszN	MWKyOEBp	NGHRU3dFVVOR	MnLsSIVkemWjc3XzJINmdGxic4Xyeol3[Wx?	NXP3Wo96OjJ7N{K2NVE>
SKLMS	MVXDfZRwfG:6aXOgRZN{[Xl?	NGfNbII4PSCwTR?=	NFLyRo06PiCq		MX3JcoR2[2W\|IHHwc5B1d3Orcx?=	NUDLVm5pOjJ6MkG5PVc>
Leio285	MlzyR5l1d3SxeHnjJGF{e2G7	NVXkb2dGPzVibl2=	NYfHWVE2QTZiaB?=		MmnFTY5lfWOnczDhdI9xfG:\|aYO=	M1PtXVIzQDJzOUm3
Mes-Sa	MkPPR5l1d3SxeHnjJGF{e2G7	NF\yUoI4PSCwTR?=	MmG0PVYhcA>?		NHzaSHFKdmS3Y3XzJIFxd3C2b4Ppdy=>	MWWyNlgzOTl7Nx?=
DAOY	MonrR5l1d3SxeHnjJGF{e2G7	NUXXbmhlOTBizszN	MV23NkBp	NGf2OXFFVVOR	M1PDeWlEPTB;MD6wOEDPxE1?	NFG3W4MzOjZ4OUOzOS=>
IMR32	MXnDfZRwfG:6aXOgRZN{[Xl?	MorqNVAh\|ryP	M3;6XFczKGh?	MlvVSG1UVw>?	M2H4eWlEPTB;MD6wN{DPxE1?	NH3wbFIzOjZ4OUOzOS=>
Molt-4	NIDtR2tEgXSxdH;4bYMhSXO\|YYm=	MonlNVAh\|ryP	NXu0WmF1PzJiaB?=	MX7EUXNQ	MXvJR\|UxRTBwMEKg{txO	Mn;XNlI3Pjl\|M{W=
MOLM-13	MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NV:1[Fg3OyEQvF2=	M4fMUlczKGh?		NEiyXIJFcW2rbnnzbIV{KGOnbHygeoli[mmuaYT5	M4DLR\|IzPDh6MkS5
HL-60	MmnoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NI\YfFU{KM7:TR?=	MV23NkBp		NUfSNIFOTGmvaX7pd4hmeyClZXzsJJZq[WKrbHn0fS=>	MVKyNlQ5QDJ2OR?=
MV4-11	MlfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MVSzJO69VQ>?	Ml7kO\|IhcA>?		MmrDSIlucW6rc3jld{Bk\WyuII\pZYJqdGm2eR?=	MoXyNlI1QDh{NEm=
SKM-1	M2rYXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NG\2cVQ{KM7:TR?=	M4LNZVczKGh?		NWfYOYRvTGmvaX7pd4hmeyClZXzsJJZq[WKrbHn0fS=>	NEDJTIozOjR6OEK0PS=>
SH2	MmDWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M1i5[\|Mh\|ryP	MWW3NkBp		MVzEbY1qdmm\|aHXzJINmdGxidnnhZoltcXS7	MlTYNlI1QDh{NEm=
NOMO-1	M330Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M4njXFMh\|ryP	Mne2O\|IhcA>?		NFS3[GNFcW2rbnnzbIV{KGOnbHygeoli[mmuaYT5	MlXHNlI1QDh{NEm=
OCL-AML2	MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MVqzJO69VQ>?	M{HiO\|czKGh?		M33KVGRqdWmwaYPo[ZMh[2WubDD2bYFjcWyrdIm=	M32yU\|IzPDh6MkS5
PL-21	NXrNTWdvT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MYizJO69VQ>?	MXe3NkBp		NFPMb4tFcW2rbnnzbIV{KGOnbHygeoli[mmuaYT5	MX:yNlQ5QDJ2OR?=
KG-1	NUmwRZV[T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MlzDN{DPxE1?	NILFWoI4OiCq		MlrDSIlucW6rc3jld{Bk\WyuII\pZYJqdGm2eR?=	MkTaNlI1QDh{NEm=
A172	NGD6PIhEgXSxdH;4bYMhSXO\|YYm=	NFXGTpcyODBizszN	MmPwNlQhcA>?	M1n2cmROW09?	Mo\QTWM2OD1yLkGyNEDPxE1?	Mnq4NlIzPzR\|OUm=
U87	NFWxb3lEgXSxdH;4bYMhSXO\|YYm=	NIntOFcyODBizszN	NXG0Nm5HOjRiaB?=	M2f1VGROW09?	NH\LVVVKSzVyPUCuNVA2KM7:TR?=	MUGyNlI4PDN7OR?=
U251	MXzDfZRwfG:6aXOgRZN{[Xl?	M37x[FExOCEQvF2=	Mmm5NlQhcA>?	M3fPS2ROW09?	NWW2NHRnUUN3ME2wMlExOCEQvF2=	NYPCSnltOjJ{N{SzPVk>
T98	NVzDd29iS3m2b4TvfIlkKEG\|c3H5	NHrvTGEyODBizszN	M1;3SFI1KGh?	M1f6RWROW09?	NF;pcnpKSzVyPUCuNVI2KM7:TR?=	MnWxNlIzPzR\|OUm=
LN18	NX3yb5l7S3m2b4TvfIlkKEG\|c3H5	Mme4NVAxKM7:TR?=	NUPSRXV4OjRiaB?=	MnP3SG1UVw>?	M1XVdWlEPTB;MD6yNVAh\|ryP	M3zSSlIzOjd2M{m5
LN443	MmDXR5l1d3SxeHnjJGF{e2G7	NYPPTY9nOTByIN88US=>	NF7OPWwzPCCq	M1;5UmROW09?	NF:zR4lKSzVyPUCuNlIxKM7:TR?=	NUPicJMzOjJ{N{SzPVk>
HF66	MYjDfZRwfG:6aXOgRZN{[Xl?	MV2xNFAh\|ryP	MWGyOEBp	NUDNZZNwTE2VTx?=	NHHaemdKSzVyPUCuNlI2KM7:TR?=	MWiyNlI4PDN7OR?=
HF2303	M1z6eGN6fG:2b4jpZ{BCe3OjeR?=	M3nkTlExOCEQvF2=	NG\OSHEzPCCq	NU\4XmJFTE2VTx?=	NInMU25KSzVyPUCuNFYxKM7:TR?=	Mm\KNlIzPzR\|OUm=
HF2359	MkTLR5l1d3SxeHnjJGF{e2G7	NWHYTlBxOTByIN88US=>	MlrSNlQhcA>?	NUfWdG1PTE2VTx?=	NX63NmJkUUN3ME2wMlA3OCEQvF2=	NVH3dW0yOjJ{N{SzPVk>
HF2414	NX3sW2oyS3m2b4TvfIlkKEG\|c3H5	MYCxNFAh\|ryP	NHTMfZEzPCCq	MVnEUXNQ	MVLJR\|UxRTBwMEiwJO69VQ>?	MXmyNlI4PDN7OR?=
A-673	NUn6cnA2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M2f5SFExKM7:TR?=	NVztTWdOQTZiaB?=	M2\tUmROW09?	NHz6WopKSzVyPUCuNFMzKM7:TR?=	MVWyNVQ1QDV7MR?=
TC-32	NIPGZllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NVvaeYh{OTBizszN	M4TC[\|k3KGh?	M1\EdWROW09?	MVzJR\|UxRTBwMEO5JO69VQ>?	NEL6NJYzOTR2OEW5NS=>
TC-71	NHnUc2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MkL5NVAh\|ryP	NYrFSXlpQTZiaB?=	NVjDN3lkTE2VTx?=	M{HPcmlEPTB;MD6xNFIh\|ryP	NHnSSGYzOTR2OEW5NS=>
SK-N-MC	M3;m[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Mle2NVAh\|ryP	NGnTR5o6PiCq	M3\ZXWROW09?	MVPJR\|UxRTBwMEeyJO69VQ>?	NXPneIlHOjF2NEi1PVE>
CHLA-9	MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NGrYUHYyOCEQvF2=	NFe2cHY6PiCq	NHPLe\|FFVVOR	MlHFTWM2OD1yLkCxPEDPxE1?	NWToZW1xOjF2NEi1PVE>
CHLA-10	MmDIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MX[xNEDPxE1?	MnPRPVYhcA>?	NWTX[3FTTE2VTx?=	MV7JR\|UxRTBwME[wJO69VQ>?	NGHoRYUzOTR2OEW5NS=>
CHLA-25	M3XqO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NHG0[VQyOCEQvF2=	MWe5OkBp	M3LlZWROW09?	M17tOmlEPTB;MD6xOlgh\|ryP	MXqyNVQ1QDV7MR?=
CHLA-32	M4D5U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NVqycG96OTBizszN	NETnNG46PiCq	MoLnSG1UVw>?	MmGxTWM2OD1yLkGzOkDPxE1?	MUGyNVQ1QDV7MR?=
CHLA-56	NWXaVmNRT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MmD1NVAh\|ryP	MXy5OkBp	NXW0dmRETE2VTx?=	MXPJR\|UxRTFyIN88US=>	MoXDNlE1PDh3OUG=
CHLA-258	NIDhfWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NYX0WFZLOTBizszN	NEfKUFQ6PiCq	MnTNSG1UVw>?	MlXDTWM2OD1yLkGzNkDPxE1?	MkXFNlE1PDh3OUG=
COG-E-352	M4H5Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M3jPSlExKM7:TR?=	MnPaPVYhcA>?	NFTidIRFVVOR	NHLI[YFKSzVyPUCuNFQ{KM7:TR?=	NFu4b3kzOTR2OEW5NS=>
CHLA-90	M{XqSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M1KxflExKM7:TR?=	NELo[446PiCq	NUez[lRHTE2VTx?=	Mo\2TWM2OD1yLkC2NUDPxE1?	M{\rXFIyPDR6NUmx
CHLA-119	NYPremJpT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MnTxNVAh\|ryP	NWi3enIzQTZiaB?=	M163dmROW09?	M{GwPGlEPTB;MD6wNlIh\|ryP	Mni0NlE1PDh3OUG=
CHLA-122	MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MliwNVAh\|ryP	NE\PdYo6PiCq	MlP6SG1UVw>?	M3nicmlEPTB;MD6wNVkh\|ryP	M1TZb\|IyPDR6NUmx
CHLA-136	NIPXT5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MUmxNEDPxE1?	MnftPVYhcA>?	NX7sem5zTE2VTx?=	NXH5eGFNUUN3ME2wMlA{QSEQvF2=	NFfOO4wzOTR2OEW5NS=>
CHLA-140	NIDFb4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NXTEUYY{OTBizszN	MUG5OkBp	NEXuWIxFVVOR	M4jod2lEPTB;MD6wNlYh\|ryP	NH7JdHczOTR2OEW5NS=>
LA-N-6	MljuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NH\qSYIyOCEQvF2=	MmjQPVYhcA>?	NX7DUmRITE2VTx?=	M2rJ[WlEPTB;MD6wOVQh\|ryP	MX:yNVQ1QDV7MR?=
NB-1643	NEHW[YFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NHj5VW0yOCEQvF2=	NHvBe5Y6PiCq	NHXYbllFVVOR	NGjjb5FKSzVyPUCuNFM4KM7:TR?=	M2\sc\|IyPDR6NUmx
NB-EBc1	NVXDWpl1T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MVmxNEDPxE1?	NEDVSWY6PiCq	NETlTnJFVVOR	MkPkTWM2OD1yLkC1NEDPxE1?	NXXqWYI5OjF2NEi1PVE>
SK-N-BE-1	NFj0S4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MVGxNEDPxE1?	NVf5SoNrQTZiaB?=	NGW3d25FVVOR	NXHUXXpjUUN3ME2wMlAzQCEQvF2=	MoLVNlE1PDh3OUG=
SK-N-BE-2	M2njbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MXuxNEDPxE1?	NX63VnJXQTZiaB?=	NXzVNop4TE2VTx?=	M4TJfGlEPTB;MD6wN\|Yh\|ryP	M4qzW\|IyPDR6NUmx
SMS-KAN	NXrXNGRmT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MoK4NVAh\|ryP	MX[5OkBp	MXHEUXNQ	M3S1S2lEPTB;MD6wN\|Qh\|ryP	M{XFW\|IyPDR6NUmx
SMS-KANR	M2rQOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Mo\uNVAh\|ryP	M{jz[Fk3KGh?	MmDtSG1UVw>?	MonmTWM2OD1yLkCyOkDPxE1?	M1v2dlIyPDR6NUmx
SMS-KCN	NHzsTpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NHLVRYcyOCEQvF2=	M1;ObVk3KGh?	NIXDXZlFVVOR	MVzJR\|UxRTBwMEG5JO69VQ>?	NIHvV2gzOTR2OEW5NS=>
SMS-KCNR	M17YcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Mn25NVAh\|ryP	NU\tOnp[QTZiaB?=	NXTUU5hkTE2VTx?=	M4LWNmlEPTB;MD6wNVAh\|ryP	NIXIRYUzOTR2OEW5NS=>
SMS-LHN	NGC5RVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MkfLNVAh\|ryP	NWjud25mQTZiaB?=	NUTZZ2ZZTE2VTx?=	Ml71TWM2OD1yLkCzNkDPxE1?	MUOyNVQ1QDV7MR?=
SMS-MSN	MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	Ml3UNVAh\|ryP	MYW5OkBp	NVXuUmxGTE2VTx?=	M{e3WWlEPTB;MD6wNlIh\|ryP	NVfqRldXOjF2NEi1PVE>
SMS-SAN	MnG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NX\lSFFROTBizszN	MVu5OkBp	MmfVSG1UVw>?	NXH4UGtEUUN3ME2wMlAzOCEQvF2=	MWCyNVQ1QDV7MR?=
Granta-4	MWXDfZRwfG:6aXOgRZN{[Xl?	MWOxNEDPxE1?	M1\YfFch\A>?		NEnJdYlKSzVyPUCuNFQxKM7:TR?=	NWT2bI9FOjF{OUG4Olc>
DB	NF3NXmREgXSxdH;4bYMhSXO\|YYm=	MX[xNEDPxE1?	MkLUO{Bl		MlP4TWM2OD1yLkC0NkDPxE1?	NXnROoIxOjF{OUG4Olc>
RL	MoTBR5l1d3SxeHnjJGF{e2G7	MVuxNEDPxE1?	NUPYb216PyCm		MVnJR\|UxRTBwMEG1JO69VQ>?	MU[yNVI6OTh4Nx?=
K562	NHnlfZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MYSxNEDPxE1?	M2[1bFk3KGh?		NHPHeWdKSzVyPUCuNFg4KM7:TR?=	MYOyNVA6OTZ\|Mx?=
LAMA-84	M3j6bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NVi0PHNwOTBizszN	MYO5OkBp		MkD5TWM2OD1yLkC1O{DPxE1?	NGSwWWkzOTB7MU[zNy=>
MM15	NXPCW5BmT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NWD2dHhbPCEQvF2=	NX;qT4ZqPzJiaB?=	M{fhTWROW09?	NH7UOpBKSzVyPUCuNVMh\|ryP	NE[1[48zODN6Mki0OC=>
OPM1	NHHocFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M{\KU\|Qh\|ryP	MWq3NkBp	MYLEUXNQ	NUjJSlJPUUN3ME2wMlA{KM7:TR?=	MlzMNlA{QDJ6NES=
RPM1	NWGw[GJUT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MVW0JO69VQ>?	MmjsO\|IhcA>?	M{\SPGROW09?	NIrXbohKSzVyPUGwMlMzKM7:TR?=	MV6yNFM5Ojh2NB?=
INA6	M3;yRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MWK0JO69VQ>?	MnyyO\|IhcA>?	NFHU[oZFVVOR	M3rSZ2lEPTB;MD6wNFIh\|ryP	NFS4RYszODN6Mki0OC=>
OPM2	MkiyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NGnac5I1KM7:TR?=	NF6y[5Y4OiCq	MnHvSG1UVw>?	NUHDXmFDUUN3ME20MlM4KM7:TR?=	NUnrTVJwOjB\|OEK4OFQ>
MM1R	NF;ae2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NX3DOZRwPCEQvF2=	Mmm5O\|IhcA>?	M{\HXGROW09?	MXrJR\|UxRTFwNkig{txO	M1\jV\|IxOzh{OES0
DOX40	Mnr1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M{Hz[lQh\|ryP	M4jnflczKGh?	M3m0TGROW09?	M{j5cGlEPTB;NT60PEDPxE1?	Ml3xNlA{QDJ6NES=
LR5	MnjHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	Ml61OEDPxE1?	NEXFWWQ4OiCq	MkGxSG1UVw>?	MmfKTWM2OD1{LkWzJO69VQ>?	NVjpNW96OjB\|OEK4OFQ>
U266	MlS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NIK5XoI1KM7:TR?=	NHyzUY44OiCq	Mln0SG1UVw>?	M37sc2lEPTB;MT60N{DPxE1?	M3n4b\|IxOzh{OES0
RD	M1jNdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NVX4TXRtOTBizszN	NFfRUpU6PiCq		MmLTTWM2OD1yLkKyPEDPxE1?	MVWyNFExQDN\|OB?=
Rh41	MkCzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MVOxNEDPxE1?	NIPmclc6PiCq		NWPpU5p2UUN3ME2wMlA6OCEQvF2=	MXGyNFExQDN\|OB?=
Rh30	MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M1ztclExKM7:TR?=	NUPNN2xzQTZiaB?=		NID5fZlKSzVyPUCuNlMxKM7:TR?=	MX:yNFExQDN\|OB?=
BT-12	M1;5e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MV:xNEDPxE1?	NHfuXI46PiCq		MXvJR\|UxRTBwME[wJO69VQ>?	MkH5NlAyODh\|M{i=
CHLA-266	NXPHPGYyT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NYTmNHI4OTBizszN	NFGwSo46PiCq		NH6yUmxKSzVyPUCuNFczKM7:TR?=	NVvENVhXOjBzMEizN\|g>
TC-71	NIHVR\|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M3\VTFExKM7:TR?=	NXO2TWFEQTZiaB?=		NFPSPGpKSzVyPUCuNVAzKM7:TR?=	MmTZNlAyODh\|M{i=
SJ-GBM2	MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MlrPNVAh\|ryP	NFfmOpU6PiCq		MXPJR\|UxRTBwMEWwJO69VQ>?	MmHDNlAyODh\|M{i=
NALM-6	NH75UGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NWHvVZlsOTBizszN	NFPnS4w6PiCq		M{fyS2lEPTB;MD6wOlIh\|ryP	MnHJNlAyODh\|M{i=
COG-LL-317	MoXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MkXRNVAh\|ryP	NX3XdpNGQTZiaB?=		M37HSGlEPTB;MD6wOFch\|ryP	MWqyNFExQDN\|OB?=
RS4-11	Mnu2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M{S4fFExKM7:TR?=	M1nEfFk3KGh?		MVjJR\|UxRTBwMEG4JO69VQ>?	NWT0NlFxOjBzMEizN\|g>
MOLT-4	NWjIPGlQT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MWqxNEDPxE1?	MWq5OkBp		NYTRSm9FUUN3ME2wMlAzPiEQvF2=	MWiyNFExQDN\|OB?=
CCRF-CEM	M4TmdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NWLkVJI{OTBizszN	MUO5OkBp		NEPlSVhKSzVyPUCuNFk1KM7:TR?=	MUWyNFExQDN\|OB?=
Kasumi-1	MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MXixNEDPxE1?	MYe5OkBp		MWjJR\|UxRTBwMUCzJO69VQ>?	NVX0NWQxOjBzMEizN\|g>
Karpas-299	NWHiXGlYT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NXLuOINEOTBizszN	M4HvXlk3KGh?		NEX3dnBKSzVyPUCuNFM5KM7:TR?=	NEL1So4zODFyOEOzPC=>
Ramos-RA1	MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MVexNEDPxE1?	NFO5bpc6PiCq		M3uzZmlEPTB;MD6xNlch\|ryP	MUmyNFExQDN\|OB?=

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Assay

Methods	Test Index	PMID
Western blot	p-AURKA(T288) / p-EIF4E(S209) / c-Myc; PubMed: 28073841 Clin Cancer Res Inhibition of AURKA with alisertib downregulated p-EIF4E (S209) and c-MYC protein levels as assayed by Western blotting. phospho-Aurora A / Aurora B; PubMed: 22863010 Cell MLN8237differentially inhibited phosphorylation of Aurora kinases. CMK cells were incubated with 0.1 µM paclitaxel for 18 hr, then DMSO or MLN8237 was added and incubated for 2 hr. The degree of phosphorylation of the Aurora kinases in each sample was determined by Western blot. H3S10P / H3K27me2 / H3K27me3 / H3K9me2 / H3AcK / H4K16Ac; PubMed: 29477140 Mol Cells THP-1 cells were treated with alisertib or DMSO for 48 h. The levels of histone modifications were detected by western blot analysis with the indicated antibodies. H3 was used as a loading control.	28073841 22863010 29477140
Growth inhibition assay	Cell viability; PubMed: 25632225 Drug Des Devel Ther PANC-1 and BxPC-3 cells were treated with ALS at concentrations ranging from 0.1 μM to 50 μM for 24 hours. The viability of PANC-1 and BxPC-3 cells determined by MTT assay. ALS, alisertib.	25632225
Immunofluorescence	acetylated α-tubulin / γ-tubulin; PubMed: 29401581 FASEB J Representative immunofluorescence (IF) image and graph in human PKD1-mutant WT9-7, WT9-12 cells or hTERT-RPE1 (RPE1) cells after 2 hours treatment with vehicle, ganetespib , or alisertib to inhibit AURKA, or combination of alisertib and ganetespib. acetylated α-tubulin (red); γ-tubulin (green); DAPI (blue). Scale bars, 5 μm. E-cadherin / β-catenin / vimentin / p-SMAD5; PubMed: 23334326 Oncogene Immunofluorescence analysis of CD24 (-/low) cells treated with1 μM MLN8237 for 48 and 72 h showing reversion of EMT. E-cadherin and p-SMAD5 were labeled in red, β-catenin and vimentin were labeled in green, and DNA was labeled in blue with Hoechst dye. Centrin-2 / tubulin; PubMed: 30899434 Oncotarget Following inhibition of Aurora A kinase activity with 100 nM alisertib, cells with two or excess centrosomes similarly exhibit disorganized mitotic spindles. Cells with extra centrosomes are efficiently clustered into bipolar spindles prior to anaphase onset while those with supernumerary centrosomes undergo multipolar mitoses. Centrin-2, a marker of centrioles is shown in green, tubulin in red, and chromatin in blue. AurA inhibitor: alisertib. phospho-Aurora A(T288); PubMed: 20382844 Blood MM1.S cells were treated with DMSO or MLN8237 (0.5μM) for 24 hours and then stained with anti-phospho (Thr288)-Aurora-A kinase antibody (red), αtubulin (green), and DNA (blue). Overlapping localization is shown in the merged images. Arrow indicates Aurora-A autophosphorylation on Thr288 in the centrosome (original magnification ×40). Magnified single mitotic cell image is shown in the right panel.	29401581 23334326 30899434 20382844

In vivo

MLN8237 significantly reduces the tumor burden with tumor growth inhibition (TGI) of 42% and 80% at 15 mg/kg and 30 mg/kg, respectively, and prolongs the survival of mice compared with the control. ^[2]

Protocol

Kinase Assay:^[1]	- Collapse Aurora A radioactive Flashplate enzyme assay: Aurora A radioactive Flashplate enzyme assay is conducted to determine the nature and degree of MLN8237-mediated inhibition in vitro. Recombinant Aurora A is expressed in Sf9 cells and purified with GST affinity chromatography. The peptide substrate for Aurora A is conjugated with biotin (Biotin-GLRRASLG). Aurora A kinase (5 nM) is assayed in 50 mM Hepes (pH 7.5), 10 mM MgCl₂, 5 mM DTT, 0.05% Tween 20, 2 μM peptide substrate, 3.3 μCi/mL [γ-³³P]ATP at 2 μM, and increasing concentrations of MLN8237 by using Image FlashPlates.
Cell Research:^[2]	- Collapse Cell lines: MM1.S, MM.1R, LR5, RPMI 8226, DOX40, OPM1, OPM2, INA6, and U266 Concentrations: Dissolved in DMSO, final concentrations ~10 μM Incubation Time: 24, 48, and 72 hours Method: Cells are exposed to various concentrations of MLN8237 for 24, 48, and 72 hours. Cells viability is measured using MTT assay, and cell proliferation is measured using ³[H]-thymidine incorporation. For cell cycle analysis, cells are permeabilized by 70% ethanol at -20 °C, and incubated with 50 μg/mL PI and 20 units/mL RNase-A. DNA content is analyzed by flow cytometry using BDFACS-Canto II and FlowJo software. For the detection of apoptosis and senescence, cells are stained with fluorescein isothiocyanate-annexin V and PI. Apoptotic cells are determined by flow cytometric analysis using BDFACS-Canto II and FlowJo software. (Only for Reference)
Animal Research:^[2]	- Collapse Animal Models: Severe combined immune-deficient (SCID) mice inoculated subcutaneously with MM1.S cells Formulation: Formulated in 10% 2-hydroxypropyl-β-cyclodextrin/1% sodium bicarbonate Dosages: ~30 mg/kg/day Administration: Orally (Only for Reference)

References

Solubility (25°C)

In vitro	DMSO	27 mg/mL (52.03 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 5%DMSO+30% PEG300+5%Tween-80+ddH2O For best results, use promptly after mixing.	8mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download Alisertib (MLN8237) SDF

Molecular Weight	518.92
Formula	C₂₇H₂₀ClFN₄O₄
CAS No.	1028486-01-2
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	N/A
Smiles	COC1=C(C(=CC=C1)F)C2=NCC3=C(N=C(NC4=CC(=C(C=C4)C(O)=O)OC)N=C3)C5=C2C=C(Cl)C=C5

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-10-14)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02812056	Withdrawn	Drug: Alisertib\|Drug: TAK-228	Malignant Neoplasms of Digestive Organs\|Malignant Neoplasms of Female Genital Organs\|Malignant Neoplasms of Lip Oral Cavity and Pharynx\|Malignant Neoplasms of Male Genital Organs	M.D. Anderson Cancer Center\|Millennium Pharmaceuticals Inc.	September 2016	Phase 1
NCT02719691	Recruiting	Drug: Alisertib\|Drug: MLN0128	Metastatic Breast Cancer\|Solid Tumors	University of Colorado Denver	May 13 2016	Phase 1
NCT02367352	Terminated	Drug: Alisertib\|Drug: Paclitaxel	Advanced Solid Tumors\|Ovarian Cancer\|Small Cell Lung Cancer	Millennium Pharmaceuticals Inc.\|Takeda	March 19 2015	Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
What is the suggested formulation of this compound for mouse injection(i.p.)?
Answer:
It can be dissolved in 6% DMSO/50% PEG 300/5% Tween 80/ddH2O at 10 mg/ml as a clear solution.

Aurora Kinase Signaling Pathway Map

Aurora Kinase Inhibitors with Unique Features

Pan Aurora Kinase Inhibitor

Danusertib (PHA-739358) : Pan-Aurora kinase inhibitor, Aurora A/B/C, IC50=13 nM/79 nM/61 nM.
Pan Aurora Kinase Inhibitor

SNS-314 Mesylate : Pan-Aurora kinase inhibitor, Aurora A/B/C, IC50=9 nM/31 nM/3 nM.
Most Potent Aurora Kinase Inhibitor

MK-5108 (VX-689) : Aurora A, IC50=0.064 nM.
Aurora Kinase Inhibitor in Clinical Trial

VX-680 (Tozasertib, MK-0457) : Phase II for Advanced Non-Small Cell Lung Cancer (NSCLC).
Classic Aurora Kinase Inhibitor

Hesperadin : Potently inhibits Aurora B with IC50 of 250 nM.

Related Aurora Kinase Products

Ro-3306 ^New

RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with K_i of 20 nM, >15-fold selectivity against a diverse panel of human kinases.
CCG-1423 ^New

CCG-1423 is a specific RhoA pathway inhibitor, which inhibits SRF-mediated transcription.
ML141 ^New

ML141 (CID-2950007), is demonstrated to be a potent, selective and reversible non-competitive inhibitor of Cdc42 GTPase suitable for in vitro assays, with IC50 of 200 nM and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7).
Barasertib (AZD1152-HQPA)

Barasertib (AZD1152-HQPA) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay, ~3700 fold more selective for Aurora B over Aurora A. Phase 1.
Tozasertib (VX-680, MK-0457)

Tozasertib (VX-680, MK-0457) is a pan-Aurora inhibitor, mostly against Aurora A with K_i_app of 0.6 nM in a cell-free assay, less potent towards Aurora B/Aurora C and 100-fold more selective for Aurora A than 55 other kinases. Phase 2.
Danusertib (PHA-739358)

Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2.
ZM 447439

ZM 447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively. It is more than 8-fold selective for Aurora A/B than MEK1, Src, Lck and has little effect against CDK1/2/4, Plk1, Chk1, etc.

Features:An Aurora selective ATP-competitive inhibitor.
MLN8054

MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of 4 nM in Sf9 insect cell. It is more than 40-fold selective for Aurora A than Aurora B. Phase 1.
MK-5108 (VX-689)

MK-5108 (VX-689) is a highly selective Aurora A inhibitor with IC50 of 0.064 nM in a cell-free assay and is 220- and 190-fold more selective for Aurora A than Aurora B/C, while it inhibits TrkA with less than 100-fold selectivity. Phase 1.
Aurora A Inhibitor I (TC-S 7010)

Aurora A Inhibitor I is a novel, potent, and selective inhibitor of Aurora A with IC50 of 3.4 nM in a cell-free assay. It is 1000-fold more selective for Aurora A than Aurora B.

Features:Aurora A Inhibitor I is a novel, potent, and selective inhibitor to Aurora A.

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Alisertib (MLN8237)