Alisertib (MLN8237)

Name: Alisertib (MLN8237)
Brand: Selleck Chemicals
SKU: S1133
Rating: 5 (210 reviews)

For research use only.

Catalog No.S1133

210 publications

CAS No. 1028486-01-2

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. Alisertib induces cell cycle arrest, apoptosis and autophagy. Phase 3.

Selleck's Alisertib (MLN8237) has been cited by 210 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, 2020, 29;11(1):2086

PubMed: 32350249 ( click the link to review the publication )

Oncogene, 2020, 16

PubMed: 32300176 ( click the link to review the publication )

Cancers (Basel), 2020, 12(3)

PubMed: 32235770 ( click the link to review the publication )

Br J Cancer, 2020, 22

PubMed: 32439932 ( click the link to review the publication )

Mol Cancer Res, 2020, 8

PubMed: 32269073 ( click the link to review the publication )

Mol Cancer Res, 2020, molcanres.1226.2019

PubMed: 32591441 ( click the link to review the publication )

Dis Model Mech, 2020, dmm.44289

PubMed: 32571902 ( click the link to review the publication )

Sci Adv, 2020, 6(29):eaba1941

PubMed: 32832623 ( click the link to review the publication )

Cancer Res, 2020, 80(16):3424-3435

PubMed: 32595135 ( click the link to review the publication )

J Cancer, 2020, 11(8):2241-2251

PubMed: 32127951 ( click the link to review the publication )

Cancer Lett, 2020, 491:50-59

PubMed: 32735909 ( click the link to review the publication )

Nucleic Acids Res, 2020, gkaa570

PubMed: 32652013 ( 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 )

Curr Biol, 2019, 29(21):3563-3578

PubMed: 31668617 ( 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

PubMed: 30778113 ( click the link to review the publication )

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

PubMed: 30844579 ( click the link to review the publication )

J Pediatr Hematol Oncol, 2019, 41(6):e359-e370

PubMed: 30702467 ( click the link to review the publication )

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

PubMed: 31429028 ( click the link to review the publication )

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

PubMed: 30899434 ( click the link to review the publication )

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

PubMed: 31698452 ( click the link to review the publication )
Nat Chem Biol, 2018, 14(8):768-777

PubMed: 29942081 ( click the link to review the publication )

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

PubMed: 30217950 ( click the link to review the publication )

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 )

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 )

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 )

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(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 )

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 )

Oncogene, 2017,

PubMed: 27593935 ( 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,

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

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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 )

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 )

Hum Mol Genet, 2016, 25(8):1574-87

PubMed: 26908596 ( 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

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

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

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Nat Commun, 2015, 6:8388

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Mol Cancer, 2015, 14(1):83

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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

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

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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(2):364-72

PubMed: ( click the link to review the publication )

Int J Mol Sci, 2015,

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

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PLoS One, 2014, 9(9):e108758

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PLoS One, 2014, 9(7):e102741

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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(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 )
Epigenetics Chromatin, 2013, 6(1):21

PubMed: 23829974 ( 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,

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 )

Oncotarget, 2011,

PubMed: 21865609 ( 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

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	M4nJSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NXTtOmF{OC53IN88US=>	NXrQRVdqPzJiaB?=	MWLEUXNQ	NFvBboxKSzVyPUCuNFQh\|ryP	NF3CSW4zPjF\|Nk[4OC=>
LS174T	Mo\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NUfJXHdvOC53IN88US=>	NVLNc4ZlPzJiaB?=	M4XsfWROW09?	MWLJR\|UxRTBwMEWg{txO	NIfJ[GQzPjF\|Nk[4OC=>
T84	MlPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NInQeFYxNjVizszN	MXG3NkBp	M4THV2ROW09?	NILrNpVKSzVyPUCuNFkh\|ryP	NV7me4dWOjZzM{[2PFQ>
LS180	NGTv[pJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NFvVZ\|IxNjVizszN	NGL1SIQ4OiCq	M1XwPGROW09?	NUS0doZ4UUN3ME2xJO69VQ>?	NWnyd2xxOjZzM{[2PFQ>
SW948	NGTacXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M3;1d\|AvPSEQvF2=	MkjoO\|IhcA>?	MWXEUXNQ	MkS2TWM2OD1zIN88US=>	MWWyOlE{PjZ6NB?=
HCT15	NXnQXI5QT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NE\hdIUxNjVizszN	MX23NkBp	NEG5dpNFVVOR	MnjITWM2ODxyLkSg{txO	MornNlYyOzZ4OES=
DLD-1	M1L1XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MmTPNE42KM7:TR?=	M2HkclczKGh?	NVHPTYhvTE2VTx?=	NFThcIRKSzVyPECuPEDPxE1?	NGS3S2IzPjF\|Nk[4OC=>
MIP-101	MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NHLqbZgxNjVizszN	MlPmO\|IhcA>?	NUfWVJRNTE2VTx?=	M2\Q[WlEPTB;MTFOwG0>	NFflNIgzPjF\|Nk[4OC=>
SNU1544	M3yzZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NYHrXo97OC53IN88US=>	NHnPV3E4OiCq	Mn3SSG1UVw>?	MWDJR\|UxRTFizszN	NX7IXGZFOjZzM{[2PFQ>
OCI-Ly10	MXHDfZRwfG:6aXOgRZN{[Xl?		M1;tO\|czKGh?	NGHlN2FFVVOR	NGH6T5ZKSzVyPUCuNFU5KM7:TR?=	MonvNlU5Pzh\|M{G=
SU-DHL2	MWfDfZRwfG:6aXOgRZN{[Xl?		M{nnTFczKGh?	MnvkSG1UVw>?	MUDJR\|UxRTBwMEGg{txO	NXXUcmdJOjV6N{izN\|E>
OCI-LY7	Ml\4R5l1d3SxeHnjJGF{e2G7		NFHuc\|E4OiCq	MnLpSG1UVw>?	M37H[2lEPTB;MD6wPFEh\|ryP	MlLsNlU5Pzh\|M{G=
SU-DHL6	MoDlR5l1d3SxeHnjJGF{e2G7		NGPHbGo4OiCq	Mli5SG1UVw>?	NYj0T3YyUUN3ME2wMlQ5OiEQvF2=	MX:yOVg4QDN\|MR?=
Jeko-1	NWXaVnRqS3m2b4TvfIlkKEG\|c3H5		NHzHWmU4OiCq	NHLRcHVFVVOR	MX\JR\|UxRTBwMEK5JO69VQ>?	M3:w[\|I2QDd6M{Ox
JVM-2	Mn3zR5l1d3SxeHnjJGF{e2G7		M371eVczKGh?	NGnKdHdFVVOR	MVrJR\|UxRTBwMEGg{txO	NX3K[nZIOjV6N{izN\|E>
Rec-1	NXH3dZZ2S3m2b4TvfIlkKEG\|c3H5		NHPaNlk4OiCq	MYjEUXNQ	NUjVWWtEUUN3ME2wMlA5PyEQvF2=	M3;ieVI2QDd6M{Ox
Z-138	M3PKXmN6fG:2b4jpZ{BCe3OjeR?=		M1;6W\|czKGh?	NGDvcpRFVVOR	M3:zbmlEPTB;MD6wNVMh\|ryP	M1PPSVI2QDd6M{Ox
H9	MmTwR5l1d3SxeHnjJGF{e2G7		MUW3NkBp	NIHPNYRFVVOR	MYfJR\|UxRTBwNjFOwG0>	MUSyOVg4QDN\|MR?=
HH	MVPDfZRwfG:6aXOgRZN{[Xl?		MVG3NkBp	M4DjRWROW09?	NWXBenVWUUN3ME2wMlch\|ryP	NYXMdXA2OjV6N{izN\|E>
DND41	NXH2SXFVS3m2b4TvfIlkKEG\|c3H5		NXj1[Jl2PzJiaB?=	NVLNOIZETE2VTx?=	M2Hx[2lEPTB;MD6xJO69VQ>?	MXSyOVg4QDN\|MR?=
CCL119	MUHDfZRwfG:6aXOgRZN{[Xl?		MlvnO\|IhcA>?	MmDLSG1UVw>?	NUXZfm1RUUN3ME2wMlA3OiEQvF2=	M2ezflI2QDd6M{Ox
J.Cam 1.6	NH7KOpREgXSxdH;4bYMhSXO\|YYm=		M1;EVFczKGh?	M{W4WmROW09?	MUjJR\|UxRTBwMUC1JO69VQ>?	NVTZV3QzOjV6N{izN\|E>
Sup-T1	NYTpTZJsS3m2b4TvfIlkKEG\|c3H5		MofXO\|IhcA>?	NYLqZoF5TE2VTx?=	MmDxTWM2OD1{LkG0NkDPxE1?	MXKyOVg4QDN\|MR?=
Tib 152	NELueW5EgXSxdH;4bYMhSXO\|YYm=		NHGwTWY4OiCq	Moe5SG1UVw>?	NFfQTYtKSzVyPUCuPEDPxE1?	Mne3NlU5Pzh\|M{G=
MCF7	NXrwb2ZMTnWwY4Tpc44hSXO\|YYm=	MkDpOUDPxE1?	M3Ht[VI1KGh?	M4LyN2ROW09?	NXXGcVJlUW6mdXPld{BIOi:PIHHydoV{fA>?	MXyyOVg{PDRyMR?=
MDA-MB-231	MUHGeY5kfGmxbjDBd5NigQ>?	MofIOUDPxE1?	NInRcoEzPCCq	MXnEUXNQ	NYmzZ3pRUW6mdXPld{BIOy:PIHHydoV{fA>?	M4nTflI2QDN2NECx
MCF7	NE\JRlVHfW6ldHnvckBCe3OjeR?=	NV;EenF6PSEQvF2=	NEnONmczPCCq	MlnMSG1UVw>?	M1z1bWRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDDSGsyN0OGQ{K=	NVL5VppvOjV6M{S0NFE>
MCF7	NGToS4xHfW6ldHnvckBCe3OjeR?=	NYXhPWJ4PSEQvF2=	M3X3NFI1KGh?	NInO[3hFVVOR	MoHmSIVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIFPET\|I>	NY\wd\|ZIOjV6M{S0NFE>
MCF7	NXv1emh3TnWwY4Tpc44hSXO\|YYm=	NH3XV\|I2KM7:TR?=	NWnaOYttOjRiaB?=	Mn[1SG1UVw>?	M1vNPGRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDjfYNtcW5iQkG=	MlrPNlU5OzR2MEG=
MCF7	M2XacWZ2dmO2aX;uJGF{e2G7	NFzDdng2KM7:TR?=	Mlq2NlQhcA>?	MX3EUXNQ	MlrLTY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIICyNUBY[WZzL1PpdFE>	NEHZR3EzPTh\|NESwNS=>
MCF7	M3uybWZ2dmO2aX;uJGF{e2G7	MojUOUDPxE1?	M2jueVI1KGh?	MXvEUXNQ	NULyRWZuUW6lcnXhd4V{KHSqZTDlfJBz\XO\|aX;uJIxmfmWuIH;mJJAzPyCNaYCx	M4DPVFI2QDN2NECx
MDA-MB-231	M3qxN2Z2dmO2aX;uJGF{e2G7	MUi1JO69VQ>?	NV3RSHBsOjRiaB?=	Mo[wSG1UVw>?	NGjPNIdF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOS:FRFOy	NHXUZpEzPTh\|NESwNS=>
MDA-MB-231	MnjtSpVv[3Srb36gRZN{[Xl?	NFryfZIyKM7:TR?=	MXmyOEBp	M2jKXmROW09?	MV\JcoNz\WG\|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiQ1TLNi=>	Mm[wNlU5OzR2MEG=
MDA-MB-231	M3e5OWZ2dmO2aX;uJGF{e2G7	NHzleXA2KM7:TR?=	MmjPNlQhcA>?	MkTwSG1UVw>?	M{jnZWRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDjfYNtcW5iQkG=	MoS4NlU5OzR2MEG=
MDA-MB-231	Mnz2SpVv[3Srb36gRZN{[Xl?	NE\kT5Q2KM7:TR?=	MXKyOEBp	M4XvZmROW09?	MXjJcoNz\WG\|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZicEKxJHdi\jFxQ3nwNS=>	NX7ONlRuOjV6M{S0NFE>
MDA-MB-231	MlnsSpVv[3Srb36gRZN{[Xl?	MkPjOUDPxE1?	MmXMNlQhcA>?	MnnUSG1UVw>?	NHzjWo5KdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gdFI4KEurcEG=	NEDS[5EzPTh\|NESwNS=>
MDA-MB-231	NIf3bYZHfW6ldHnvckBCe3OjeR?=	MXq1JO69VQ>?	MmX4NlQhcA>?	Mo\ISG1UVw>?	MmSxTY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIIC1Ny=>	NWjENnBpOjV6M{S0NFE>
MCF7	NUTselFLSXCxcITvd4l{KEG\|c3H5	MVK1JO69VQ>?	NH22[W8zPCCq	M3LpcGROW09?	NHf4PGVKdmS3Y3XzJIFxd3C2b4TpZ{Bl\WG2aB?=	MYCyOVg{PDRyMR?=
MDA-MB-231	NIW4e2tCeG:ydH;zbZMhSXO\|YYm=	MlHPOUDPxE1?	NHvNTI0zPCCq	MVfEUXNQ	NUDHWIR7UW6mdXPld{BieG:ydH;0bYMh\GWjdHi=	NX3XUVVDOjV6M{S0NFE>
MCF7	NWLlV4V1TnWwY4Tpc44hSXO\|YYm=	M{jHUlEh\|ryP	NYewWmg2PzJiaB?=	MXrEUXNQ	NHS4WYdKdmS3Y3XzJIF2fG:yaHHnbYMh\GWjdHi=	MnHuNlU5OzR2MEG=
MDA-MB-231	NWThRmY6TnWwY4Tpc44hSXO\|YYm=	NUn2WJJqOSEQvF2=	M3faNVczKGh?	M{jmcmROW09?	M4nTdmlv\HWlZYOgZZV1d3CqYXfpZ{Bl\WG2aB?=	MWCyOVg{PDRyMR?=
U-2 OS	NWW1[plLT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M1P2d\|UxKM7:TR?=	MnnFNlQhcA>?	NFTaW\|VFVVOR	MVvJR\|UxRTF4Lk[g{txO	NIPVUWIzPTd7MkixNS=>
MG-63	NVLjeGhNT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NHHDU\|g2OCEQvF2=	NVSyU2l{OjRiaB?=	NInz[5hFVVOR	NV;sbnJuUUN3ME25MlUh\|ryP	M4XUNVI2Pzl{OEGx
U-2 OS	M4n5PWFxd3C2b4Ppd{BCe3OjeR?=	NULIeWJ1PSEQvF2=	M1voT\|I1KGh?	NIjQV5hFVVOR	NEnJWmlKdmS3Y3XzJIFxd3C2b4TpZ{Bk\WyuIHTlZZRp	M2K0WVI2Pzl{OEGx
MG-63	NF\oPYpCeG:ydH;zbZMhSXO\|YYm=	MVO1JO69VQ>?	MkPYNlQhcA>?	M3HQNmROW09?	M1vvemlv\HWlZYOgZZBweHSxdHnjJINmdGxiZHXheIg>	M3zjbFI2Pzl{OEGx
U-2 OS	MlH0SpVv[3Srb36gRZN{[Xl?	M1fqdVUh\|ryP	NVTiOmZjOjRiaB?=	M3LLTWROW09?	MVzQdo9ud3SnczDheZRweGijZ3njJINmdGxiZHXheIg>	NGTDRnAzPTd7MkixNS=>
MG-63	NVPoVoM5TnWwY4Tpc44hSXO\|YYm=	MnzpOUDPxE1?	NGTkPHczPCCq	MnfpSG1UVw>?	NVewbpZoWHKxbX;0[ZMh[XW2b4DoZYdq[yClZXzsJIRm[XSq	M1S2SlI2Pzl{OEGx
PANC-1	MmjCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NUfLOYdNPTBizszN	NGTmdZQzPCCq	M{LydmROW09?	NV;JZldjUUN3ME23MlEh\|ryP	NX3EWnE6OjV4M{KyNlU>
BxPC-3	NH72TI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M3zy[lUxKM7:TR?=	M{\zNlI1KGh?	M{nHe2ROW09?	MWfJR\|UxRTZwODFOwG0>	NEW2b4gzPTZ\|MkKyOS=>
PANC-1	NFHVfYRHfW6ldHnvckBCe3OjeR?=	MlnpOUDPxE1?	NXLKe45UOjRiaB?=	MVjEUXNQ	NITtO21KdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIlvKEd{L12gdIhie2V?	M4WxRVI2PjN{MkK1
BxPC-3	MX\GeY5kfGmxbjDBd5NigQ>?	NXH5elRVPSEQvF2=	NUjPNphPOjRiaB?=	MYDEUXNQ	MnTvTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW\|dDDpckBIOi:PIIDoZZNm	NEHvZmgzPTZ\|MkKyOS=>
PANC-1	NVXub2xETnWwY4Tpc44hSXO\|YYm=	MYq1JO69VQ>?	NI\NbWQzPCCq	NEfOPWRFVVOR	MknETY5lfWOnczDheZRweGijZ3njJINmdGxiZHXheIg>	NVjCZWN3OjV4M{KyNlU>
BxPC-3	Mof1SpVv[3Srb36gRZN{[Xl?	NGrnNVI2KM7:TR?=	MYOyOEBp	NGCzTIdFVVOR	NInGTZVKdmS3Y3XzJIF2fG:yaHHnbYMh[2WubDDk[YF1cA>?	NVf6dZRsOjV4M{KyNlU>
SKOV3	MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MlftNVAxKM7:TR?=	MWOyOEBp	NV\FTolLTE2VTx?=	MlX5TWM2OD1{MD60PEDPxE1?	MXSyOVYzPDd3MB?=
OVCAR4	NIPJZXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NYPXeGxOOTByIN88US=>	MoDnNlQhcA>?	NYW3d2tYTE2VTx?=	NF75WY5KSzVyPUKyMlE{KM7:TR?=	M{\PTlI2PjJ2N{Ww
SKOV3	Mof0SpVv[3Srb36gRZN{[Xl?	MljjOUDPxE1?	NIL5bZA4OiCq	M2XkemROW09?	MYrJcoR2[2W\|IFeyM20h[XK{ZYP0	M{nCe\|I2PjJ2N{Ww
OVCAR4	M3TtcWZ2dmO2aX;uJGF{e2G7	NGT4OFI2KM7:TR?=	MUO3NkBp	NELTUoNFVVOR	M1rCeWlv\HWlZYOgS\|IwVSCjcoLld5Q>	NFLCcVkzPTZ{NEe1NC=>
SKOV3	MV7BdI9xfG:\|aYOgRZN{[Xl?	M1nZb\|Uh\|ryP	NEXBW4QzPCCq	M4nuU2ROW09?	MnLYTY5lfWOnczDhdI9xfG:\|aYO=	NHPiO28zPTZ{NEe1NC=>
OVCAR4	M4TyV2Fxd3C2b4Ppd{BCe3OjeR?=	MUK1JO69VQ>?	NUjwblB6OjRiaB?=	NIPXZWFFVVOR	NWDqSGZQUW6mdXPld{BieG:ydH;zbZM>	NET1ZWUzPTZ{NEe1NC=>
AGS	M2rNVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MoLwNlUh\|ryP	NYr5UXgyOjRiaB?=	NYqxWFBzTE2VTx?=	NWTtRnJwUUN3ME2xPU4xQSEQvF2=	NVriVWJxOjV4MEm5NlM>
NCI-N78	NXHCbGVzT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NXHjfZczOjVizszN	NWD2U\|FvOjRiaB?=	NVnVPYJkTE2VTx?=	M1XlXWlEPTB;Mk[uN\|Mh\|ryP	MoqxNlU3ODl7MkO=
AGS	M3nFNmFxd3C2b4Ppd{BCe3OjeR?=	NEO5RY02KM7:TR?=	NGixVogzPCCq	MlPvSG1UVw>?	NHmwTXRKdmS3Y3XzJIFxd3C2b4Ppdy=>	NUHCfHJyOjV4MEm5NlM>
NCI-N78	MXrBdI9xfG:\|aYOgRZN{[Xl?	Mki1OUDPxE1?	MoP4NlQhcA>?	MVLEUXNQ	MoXZTY5lfWOnczDhdI9xfG:\|aYO=	MUWyOVYxQTl{Mx?=
AGS	MlzISpVv[3Srb36gRZN{[Xl?	NFn1Z2U2KM7:TR?=	NUP5dY8{OjRiaB?=	NFLrNpZFVVOR	MmP3TY5lfWOnczD0bIUh[XW2b4DoZYd6	MVuyOVYxQTl{Mx?=
NCI-N78	M{myfmZ2dmO2aX;uJGF{e2G7	NF\MWHg2KM7:TR?=	NUO0bIVqOjRiaB?=	M4XDVmROW09?	NXj0XpZRUW6mdXPld{B1cGViYYX0c5Bp[We7	MkL6NlU3ODl7MkO=
HSC-3	Mmj3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M33zWFEh\|ryP	MXe0PEBp		M3i4NmlEPTB;MD61OEDPxE1?	MUWyOVM3PjF2Mx?=
GB30	MkDCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MWWxJO69VQ>?	MoH2O{Bl	NH\mSYZFVVOR	MVTJR\|UxRTBwMEGxJO69VQ>?	MYeyOVExPjR{OB?=
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GB169	NInteHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M{ThclEh\|ryP	NWSxN4J7PyCm	M4GzfGROW09?	MWHJR\|UxRTBwMEOyJO69VQ>?	MknoNlUyODZ2Mki=
T24	Ml23SpVv[3Srb36gRZN{[Xl?	NE\SWIQyKM7:TR?=	Mk\MOFghcA>?	M13ZSGROW09?	NIPFTHhKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0	MViyN\|QxOzZ\|Mx?=
RT4	NXnZSGhtTnWwY4Tpc44hSXO\|YYm=	MnzFNUDPxE1?	Mm\1OFghcA>?	MkG4SG1UVw>?	MVrJcoR2[2W\|IHPlcIwh[3mlbHWgZZJz\XO2	NIrycVIzOzRyM{[zNy=>
UM-UC-3	M3;BVmZ2dmO2aX;uJGF{e2G7	NGDkbY4yKM7:TR?=	NFvDV\|M1QCCq	MnTvSG1UVw>?	MXPJcoR2[2W\|IHPlcIwh[3mlbHWgZZJz\XO2	NIntenUzOzRyM{[zNy=>
T24	NV2yU5l5SXCxcITvd4l{KEG\|c3H5	NG\Qd2g{NjF4IN88US=>	NFnJepE6PiCq	NVHrZoNXTE2VTx?=	NFzFTmtKSzVyPUCuNFMxPiEQvF2=	NFH3eXYzOzRyM{[zNy=>
RT4	MX\BdI9xfG:\|aYOgRZN{[Xl?	MoHwN{4yPiEQvF2=	NV;nOW4zQTZiaB?=	MV3EUXNQ	MoOzTWM2OD1yLkGxPVgh\|ryP	M1m2[lI{PDB\|NkOz
UM-UC-3	M3zwSWFxd3C2b4Ppd{BCe3OjeR?=	MV[zMlE3KM7:TR?=	NXTaXGh4QTZiaB?=	M4rmXWROW09?	MoXFTWM2OD1yLkC0OFkh\|ryP	MYCyN\|QxOzZ\|Mx?=
OVCAR-5	NWrjcW5LTnWwY4Tpc44hSXO\|YYm=	Mo\GOVAhdk1?			NFm4Ro9KdmirYnn0d{Bk\WyuIH3p[5JifGmxbh?=	MV2yN\|M{PDN{Nx?=
SKOV3ip2	NYn6dpFOTnWwY4Tpc44hSXO\|YYm=	Mne5OVAhdk1?			MVzJcohq[mm2czDj[YxtKG2rZ4LheIlwdg>?	NWnpbHFnOjN\|M{SzNlc>
S462	NEfqPFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MUSxNFAh\|ryP	NYjOTJVMPzJiaB?=	MVXEUXNQ	M1fWU2F1fGWwdXH0[ZMh[2WubDDndo94fGh?	NVGzUWV1OjN\|MkixNVQ>
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2885	NFjrTpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NWrHVXc5OTByIN88US=>	M2n2UlczKGh?	MXLEUXNQ	NFLneIlCfHSnboXheIV{KGOnbHyg[5Jwf3Sq	M{Lx[lI{OzJ6MUG0
CRL-2396	MkS1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MX[xNFAh\|ryP		M{jxeJdifGW{	NVXqPVlyUUN3ME2wMlA6OiEQvF2=	NH3LeGMzOzF3M{WyOC=>
TIB-48	MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MWKxNFAh\|ryP		NVjpXlN4f2G2ZYK=	NU\rTWdyUUN3ME2wMlA5QCEQvF2=	MUOyN\|E2OzV{NB?=
CRL-2396	MknkR5l1d3SxeHnjJGF{e2G7	MoHTNUDPxE1?	M4DYcFQ5KGh?	NY\jNXp7f2G2ZYK=	NVjHZnBtUW6mdXPld{BieG:ydH;zbZM>	NI\zZ40zOzF3M{WyOC=>
TIB-48	MoXxR5l1d3SxeHnjJGF{e2G7	MkXsNUDPxE1?	Mn:1OFghcA>?	MkDEe4F1\XJ?	NEj6UFJKdmS3Y3XzJIFxd3C2b4Ppdy=>	NFj2bFIzOzF3M{WyOC=>
AGS	NIjzSllEgXSxdH;4bYMhSXO\|YYm=	M4DTNVAvPSEQvF2=	MWiyOEBp	NGPyOY1FVVOR	M2DzT2Rm[3KnYYPld{Bk\WyuIIP1dpZqfmGu	MW[yNlk4OjZzMR?=
FLO-1	MmDNR5l1d3SxeHnjJGF{e2G7	M2nEb\|AvPSEQvF2=	NVvPOFVLOjRiaB?=	MULEUXNQ	M13Hd2Rm[3KnYYPld{Bk\WyuIIP1dpZqfmGu	Mlu5NlI6PzJ4MUG=
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Leio285	NXH1NZE{S3m2b4TvfIlkKEG\|c3H5	M2fMPVc2KG6P	NH;uNIY6PiCq		NYXDfGJbUW6mdXPld{BieG:ydH;zbZM>	MmrzNlI5OjF7OUe=
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Molt-4	MX3DfZRwfG:6aXOgRZN{[Xl?	NH72WmQyOCEQvF2=	NXzmUItCPzJiaB?=	MoLkSG1UVw>?	MUfJR\|UxRTBwMEKg{txO	Mn;LNlI3Pjl\|M{W=
MOLM-13	NIj4SW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NHvFN2k{KM7:TR?=	MVy3NkBp		NGnBcXhFcW2rbnnzbIV{KGOnbHygeoli[mmuaYT5	M3ThcFIzPDh6MkS5
HL-60	M1qxbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NYfRbHlGOyEQvF2=	NXnKco9YPzJiaB?=		NFjoVYpFcW2rbnnzbIV{KGOnbHygeoli[mmuaYT5	MVWyNlQ5QDJ2OR?=
MV4-11	MnnZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MlL5N{DPxE1?	MoXDO\|IhcA>?		MY\EbY1qdmm\|aHXzJINmdGxidnnhZoltcXS7	NVvKPJhuOjJ2OEiyOFk>
SKM-1	M{\MWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NGLJPIY{KM7:TR?=	NVXseohsPzJiaB?=		MWfEbY1qdmm\|aHXzJINmdGxidnnhZoltcXS7	NUXrNnoyOjJ2OEiyOFk>
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NOMO-1	MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NXy3TZgzOyEQvF2=	NEO1NXA4OiCq		NEjEWGtFcW2rbnnzbIV{KGOnbHygeoli[mmuaYT5	M2XrOlIzPDh6MkS5
OCL-AML2	NUDUWIpOT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NHrLdZU{KM7:TR?=	Ml3HO\|IhcA>?		NGe4PXVFcW2rbnnzbIV{KGOnbHygeoli[mmuaYT5	NXviUm5kOjJ2OEiyOFk>
PL-21	NXzKNFhYT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	Ml3FN{DPxE1?	MlLwO\|IhcA>?		MlGxSIlucW6rc3jld{Bk\WyuII\pZYJqdGm2eR?=	NX7OOmkzOjJ2OEiyOFk>
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A172	NYrycIM6S3m2b4TvfIlkKEG\|c3H5	MnjJNVAxKM7:TR?=	M3zm[lI1KGh?	NWLD[HloTE2VTx?=	MY\JR\|UxRTBwMUKwJO69VQ>?	MkPuNlIzPzR\|OUm=
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T98	MWTDfZRwfG:6aXOgRZN{[Xl?	NF\6[4wyODBizszN	NVuzfphqOjRiaB?=	MlzwSG1UVw>?	NWLh[pV6UUN3ME2wMlEzPSEQvF2=	M4S0R\|IzOjd2M{m5
LN18	NXT4doVES3m2b4TvfIlkKEG\|c3H5	NFvLWZoyODBizszN	Mmm3NlQhcA>?	MXLEUXNQ	NUDWU4d4UUN3ME2wMlIyOCEQvF2=	MVOyNlI4PDN7OR?=
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HF2303	MXzDfZRwfG:6aXOgRZN{[Xl?	MX6xNFAh\|ryP	MnLoNlQhcA>?	MYTEUXNQ	M4rrOmlEPTB;MD6wOlAh\|ryP	NYXMdok1OjJ{N{SzPVk>
HF2359	MnG4R5l1d3SxeHnjJGF{e2G7	MmTrNVAxKM7:TR?=	NI[wT5kzPCCq	MXXEUXNQ	M4LMeGlEPTB;MD6wOlAh\|ryP	NEXxcGUzOjJ5NEO5PS=>
HF2414	NFXEfGZEgXSxdH;4bYMhSXO\|YYm=	NXmyRpFqOTByIN88US=>	NGHB[ZIzPCCq	MmHoSG1UVw>?	MV\JR\|UxRTBwMEiwJO69VQ>?	M{jkVVIzOjd2M{m5
A-673	MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NHS0VJUyOCEQvF2=	MoDwPVYhcA>?	NXLD[4NHTE2VTx?=	NUS1XphwUUN3ME2wMlA{OiEQvF2=	M3n0R\|IyPDR6NUmx
TC-32	M{\EbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MXGxNEDPxE1?	MV65OkBp	NVrWbZpyTE2VTx?=	NGrp[3VKSzVyPUCuNFM6KM7:TR?=	NUPjO5BMOjF2NEi1PVE>
TC-71	NVuwS21KT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M1TiUFExKM7:TR?=	M2DL[lk3KGh?	NFjRW5dFVVOR	MWDJR\|UxRTBwMUCyJO69VQ>?	M2jMcFIyPDR6NUmx
SK-N-MC	NYHVbWZmT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MofyNVAh\|ryP	NULCTlAyQTZiaB?=	NIHXUnpFVVOR	M3PkbGlEPTB;MD6wO\|Ih\|ryP	NEjn[oszOTR2OEW5NS=>
CHLA-9	NIfEXIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NV36fmhbOTBizszN	NXHI[YY6QTZiaB?=	NVviUllUTE2VTx?=	MV\JR\|UxRTBwMEG4JO69VQ>?	MVyyNVQ1QDV7MR?=
CHLA-10	MnzjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NEG1Nm8yOCEQvF2=	MnfRPVYhcA>?	Ml7QSG1UVw>?	M4TVdWlEPTB;MD6wOlAh\|ryP	M{TsV\|IyPDR6NUmx
CHLA-25	NVfOWpd5T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MoDjNVAh\|ryP	MlLSPVYhcA>?	Mor1SG1UVw>?	NX\oeZl5UUN3ME2wMlE3QCEQvF2=	NYXsSWo2OjF2NEi1PVE>
CHLA-32	MkXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NXi5SW1xOTBizszN	NYjEO4ZMQTZiaB?=	MWPEUXNQ	MWLJR\|UxRTBwMUO2JO69VQ>?	M4HyO\|IyPDR6NUmx
CHLA-56	NFzaVVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NXzjXFdLOTBizszN	NHjQWos6PiCq	M3[wVWROW09?	MXfJR\|UxRTFyIN88US=>	MYKyNVQ1QDV7MR?=
CHLA-258	NXfOPG9wT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M{LVTVExKM7:TR?=	NXPJRY9SQTZiaB?=	NUO0XoNpTE2VTx?=	MkHLTWM2OD1yLkGzNkDPxE1?	NHm0XJQzOTR2OEW5NS=>
COG-E-352	M2LEVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NIDtV5QyOCEQvF2=	M1LyeVk3KGh?	NWn6OlFNTE2VTx?=	MYLJR\|UxRTBwMESzJO69VQ>?	MlzMNlE1PDh3OUG=
CHLA-90	M2Gy[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M1vpclExKM7:TR?=	NF7idW46PiCq	NIrYTpBFVVOR	MWfJR\|UxRTBwME[xJO69VQ>?	MVeyNVQ1QDV7MR?=
CHLA-119	NVzqWGdUT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MojmNVAh\|ryP	NGrUeFg6PiCq	M125OWROW09?	Mkf1TWM2OD1yLkCyNkDPxE1?	MoKyNlE1PDh3OUG=
CHLA-122	MoT0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M3;UW\|ExKM7:TR?=	MYG5OkBp	NVGwOZVwTE2VTx?=	NIrEVmJKSzVyPUCuNFE6KM7:TR?=	M{CzdlIyPDR6NUmx
CHLA-136	M{PYeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Mn71NVAh\|ryP	Mlm2PVYhcA>?	M3vKS2ROW09?	MoOxTWM2OD1yLkCzPUDPxE1?	MoewNlE1PDh3OUG=
CHLA-140	MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NEDqdVIyOCEQvF2=	Mn6wPVYhcA>?	Mmq5SG1UVw>?	NHO4bFBKSzVyPUCuNFI3KM7:TR?=	NGT0R3AzOTR2OEW5NS=>
LA-N-6	NV7TU3pvT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NVjP[ZBMOTBizszN	MoHVPVYhcA>?	M{W0VGROW09?	NWP2WIhKUUN3ME2wMlA2PCEQvF2=	NFLr[IQzOTR2OEW5NS=>
NB-1643	MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MmDNNVAh\|ryP	NIqzcpA6PiCq	MmrxSG1UVw>?	MoHwTWM2OD1yLkCzO{DPxE1?	MkXDNlE1PDh3OUG=
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SK-N-BE-1	MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NHfYeZkyOCEQvF2=	MV:5OkBp	NHv4enRFVVOR	MofsTWM2OD1yLkCyPEDPxE1?	NXHCbFZTOjF2NEi1PVE>
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SMS-KAN	NV;MUmZvT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NUnKS\|JPOTBizszN	NYjYeXY2QTZiaB?=	NIrq[IRFVVOR	MUXJR\|UxRTBwMEO0JO69VQ>?	MWOyNVQ1QDV7MR?=
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Granta-4	MUfDfZRwfG:6aXOgRZN{[Xl?	MWqxNEDPxE1?	NWXUNm02PyCm		MYfJR\|UxRTBwMESwJO69VQ>?	NU\WfZF[OjF{OUG4Olc>
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LAMA-84	NVTBV3h4T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MkPxNVAh\|ryP	MWm5OkBp		MlLETWM2OD1yLkC1O{DPxE1?	MnzHNlExQTF4M{O=
MM15	M2LrWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MnznOEDPxE1?	MWG3NkBp	M17yUGROW09?	NVL3PWpTUUN3ME2wMlE{KM7:TR?=	M1myVlIxOzh{OES0
OPM1	MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MXe0JO69VQ>?	NI\R[4o4OiCq	MljZSG1UVw>?	NYW5bItmUUN3ME2wMlA{KM7:TR?=	MX2yNFM5Ojh2NB?=
RPM1	NFf2OFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NIfGPIQ1KM7:TR?=	MYK3NkBp	MYTEUXNQ	M3XUV2lEPTB;MUCuN\|Ih\|ryP	M1HWcVIxOzh{OES0
INA6	NFr5do9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M4nlclQh\|ryP	MojiO\|IhcA>?	Ml;KSG1UVw>?	Mo\QTWM2OD1yLkCwNkDPxE1?	MVeyNFM5Ojh2NB?=
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BT-12	M3j1fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MXixNEDPxE1?	NF7aTWc6PiCq		M3\ydmlEPTB;MD6wOlAh\|ryP	NEjieoMzODFyOEOzPC=>
CHLA-266	MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NXX3fpVMOTBizszN	M1vPb\|k3KGh?		Mli1TWM2OD1yLkC3NkDPxE1?	MoPpNlAyODh\|M{i=
TC-71	NF[4dnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M4DoRVExKM7:TR?=	NX[3N3I4QTZiaB?=		NEG3[oRKSzVyPUCuNVAzKM7:TR?=	MnTCNlAyODh\|M{i=
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NALM-6	M3L5U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M1XDd\|ExKM7:TR?=	NIDrbJk6PiCq		M3PPcWlEPTB;MD6wOlIh\|ryP	NV\CSHhmOjBzMEizN\|g>
COG-LL-317	NHHjd\|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NYfrPHlXOTBizszN	Ml7oPVYhcA>?		MYDJR\|UxRTBwMES3JO69VQ>?	NHvGXVAzODFyOEOzPC=>
RS4-11	NFvpSlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M1v0eVExKM7:TR?=	NFHK[nU6PiCq		NIjGW5lKSzVyPUCuNFE5KM7:TR?=	MV2yNFExQDN\|OB?=
MOLT-4	NW\B[HU{T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MnvONVAh\|ryP	MXG5OkBp		Mo\zTWM2OD1yLkCyOkDPxE1?	MYeyNFExQDN\|OB?=
CCRF-CEM	M3m0[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MoThNVAh\|ryP	NGfaNIM6PiCq		Mn3iTWM2OD1yLkC5OEDPxE1?	NGS3clgzODFyOEOzPC=>
Kasumi-1	M1i3SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NIq4[ZAyOCEQvF2=	NIq5RVc6PiCq		MoDtTWM2OD1yLkGwN{DPxE1?	NVjReFlNOjBzMEizN\|g>
Karpas-299	MojRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MUCxNEDPxE1?	MYK5OkBp		MYXJR\|UxRTBwMEO4JO69VQ>?	Mo\iNlAyODh\|M{i=
Ramos-RA1	NH75PIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M125[VExKM7:TR?=	NW\pWm41QTZiaB?=		MmXLTWM2OD1yLkGyO{DPxE1?	M4rzXFIxOTB6M{O4

... Click to View More Cell Line Experimental Data

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 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 2 years-80°C in solvent
Synonyms	N/A
Smiles	COC1=C(C(=CC=C1)F)C2=NCC3=CN=C(N=C3C4=C2C=C(C=C4)Cl)NC5=CC(=C(C=C5)C(=O)O)OC

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Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2020-09-01)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04479306	Recruiting	Drug: Alisertib\|Drug: Osimertinib\|Drug: Sapanisertib	EGFR T790M Mutation Positive Non-Small Cell Lung Carcinoma\|Recurrent Lung Non-Small Cell Carcinoma\|Stage IIIB Lung Cancer AJCC v8\|Stage IV Lung Cancer AJCC v8\|Stage IVA Lung Cancer AJCC v8\|Stage IVB Lung Cancer AJCC v8	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)	June 18 2020	Phase 1
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

Tel: +1-832-582-8158 Ext:3

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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. RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis.
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). ML141 is associated with an increase in p38 activation and may induce p38-dependent apoptosis/senescence. ML141 also protects neuroblastoma cells from metformin-induced apoptosis.
Barasertib (AZD1152-HQPA)

Barasertib (AZD1152-HQPA, AZD2811) 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. The only exceptions are Fms-related tyrosine kinase-3 (FLT-3) and c-ABL tyrosine kinase, which are inhibited by the Tozasertib with Ki of 30 nM and 20 nM, respectively. Tozasertib induces apoptosis and autophagy. 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. Danusertib induces apoptosis, cell cycle arrest, and autophagy. 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. MK-5108 (VX-689) induces autophagy. Phase 1.
Aurora A Inhibitor I (TC-S 7010)

Aurora A Inhibitor I (TC-S 7010) 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. Aurora A Inhibitor I (TC-S 7010) triggers apoptosis through the ROS-mediated UPR signaling pathway.

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

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Alisertib (MLN8237)