Osimertinib (AZD9291)

Name: Osimertinib (AZD9291)
Brand: Selleck Chemicals
SKU: S7297
Rating: 5 (221 reviews)

For research use only.

Catalog No.S7297 Synonyms: Mereletinib

221 publications

Osimertinib (AZD9291) Chemical Structure

CAS No. 1421373-65-0

Osimertinib (AZD9291) is an oral, irreversible, and mutant-selective EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells, respectively. Phase 3.

Selleck's Osimertinib (AZD9291) has been cited by 221 publications

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Nat Med, 2019, 25(1):111-118

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Cell Rep, 2021, 34(3):108647

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Mol Cancer, 2021, 20(1):17

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EBioMedicine, 2021, 64:103220

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Oncogenesis, 2021, 10(3):29

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Biochim Biophys Acta Mol Cell Res, 2021, 1868(6):119016

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Acta Pharmacol Sin, 2021, 10.1038/s41401-020-00577-1

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Toxicol Appl Pharmacol, 2021, 419:115518

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Thorac Cancer, 2021, 10.1111/1759-7714.13931

PubMed: 33710795 ( click the link to review the publication )

Oncol Lett, 2021, 21(5):418

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Transl Lung Cancer Res, 2021, 10(1):128-142

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Lung Cancer, 2021, 154:84-91

PubMed: 33631449 ( click the link to review the publication )

EBioMedicine, 2021, 64:103220

PubMed: 33529999 ( click the link to review the publication )

Nat Nanotechnol, 2021, 10.1038/s41565-021-00872-w

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Acta Neuropathol, 2020, 17

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Nat Commun, 2020, 11(1):4607

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Sci Immunol, 2020, 31;5(43) pii: eaav3937

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EMBO Mol Med, 2020, e11099

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Cancer Res, 2020, 80(21):4655-4667

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Oncogene, 2020, 10.1038/s41388-020-01497-4

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Cancer Lett, 2020, 28;483:46-58

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Cancers (Basel), 2020, 13(1)E111

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Cell Death Dis, 2020, 14;11(4):230

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Br J Cancer, 2020, 22

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Signal Transduct Target Ther, 2020, 5(1):214

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Cancer Discov, 2020, 15 pii: CD-20-0116

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Hum Mol Genet, 2020, ddaa268

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Cancer Sci, 2020, 111(10):3813-3823

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Lung Cancer, 2020, 5;145:48-57

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Mol Cancer Res, 2020, 10.1158/1541-7786.MCR-20-0664

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Front Oncol, 2020, 9:1503

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J Cell Mol Med, 2020, 10.1111/jcmm.16135

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Sci Rep, 2020, 17;10(1):2735

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Ann Transl Med, 2020, 8(6):366

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Environ Toxicol, 2020, 10.1002/tox.22899

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Biochem Biophys Res Commun, 2020, 534:1-7

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J Oncol, 2020, 17;2020:6249829

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Hum Cell, 2020, 10.1007/s13577-020-00420-z

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J Med Invest, 2020, 67(3.4):343-350

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J Hematol Oncol, 2020, 13(1):169

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Cancer Sci, 2020, 111(7):2374-2384

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Nat Cancer, 2020, 1(3):359-369

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Front Cell Dev Biol, 2020, 8:652

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Pharmaceutics, 2020, 12(10)E939

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Cells, 2020, 9(12)E2596

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Acta Pharmacol Sin, 2020, 10.1038/s41401-020-0443-1

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Mol Cancer Res, 2020, 18(4):549-559

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Physiol Rep, 2020, 8(13):e14490

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Acta Pharmacol Sin, 2020, 10.1038/s41401-020-0457-8

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Sci Rep, 2020, 10(1):11236

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Food Funct, 2020, 11(3):2714-2724

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Viruses, 2020, 12(11)E1294

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Rapid Commun Mass Spectrom, 2020, 10.1002/rcm.8955

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J Thorac Oncol, 2020, 15(5):752-765

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Nat Commun, 2019, 10(1):2701

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J Thorac Oncol, 2019, 14(4):656-671

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Clin Cancer Res, 2019, 25(11):3329-3340

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Neuro Oncol, 2019, 10.1093/neuonc/noz206

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Cell Syst, 2019, 8(2):97-108

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Cell Syst, 2019, 10.1016/j.cels.2019.10.002

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Biomaterials, 2019, 219:119400

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Cancer Res, 2019, 10.1158/0008-5472.CAN-18-2808

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Int J Cancer, 2019, 145(5):1432-1444

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Oncogene, 2019, 38(5):656-670

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Oncogene, 2019, 38(37):6399-6413

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J Exp Clin Cancer Res, 2019, 38(1):481

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Cancers, 2019, 11(3)

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Signal Transduct Target Ther, 2019,

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Acta Pharm Sin B, 2019, 9(6):1193-1203

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Mol Cancer Ther, 2019, 18(1):112-126

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Mol Cancer Ther, 2019, 18(9):1593-1601

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Am J Cancer Res, 2019, 9(8):1708-1721

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Lung Cancer, 2019, 127:146-152

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Lung Cancer, 2019, 137:85-93

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Cancer Sci, 2019, 110(11):3584-3594

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J Cell Mol Med, 2019, 23(11):7427-7437

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Sci Rep, 2019,

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Clin Lung Cancer, 2019, 20(3):167-177

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Int J Biol Sci, 2019, 15(12):2607-2614

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Respir Res, 2019, 20(1-:270

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Cancer Manag Res, 2019, 11:3419-3432

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Ann Transl Med, 2019, 7(22):651

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Toxicol Appl Pharmacol, 2019, 379:114662

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J Cell Biochem, 2019, 120(1):756-767

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Cell Biosci, 2019, 9:60

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Oncol Rep, 2019, 41(2):1059-1066

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Biomed Res Int, 2019, 2019:3129748

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Thorac Cancer, 2019, 10(10):1868-1878

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Breast Cancer (Dove Med Press), 2019, 11:231-241

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Oncol Lett, 2019, 18(1):955-961

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FEBS Open Bio, 2019, 9(10):1689-1704

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Cell Mol Gastroenterol Hepatol, 2019, 7(1):161-184

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J Thorac Oncol, 2019, 14(9):1556-1566

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JCI Insight, 2019, 4(21)

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Oncotarget, 2019, 10(26):2546-2560

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Sci Rep, 2019, 9(1):5692

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Transl Lung Cancer Res, 2019, 8(4):340-351

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Zhongguo Fei Ai Za Zhi, 2019, 22(5):264-270

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Nat Biomed Eng, 2018, 2(4):239-253

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Nat Commun, 2018, 9(1):4655

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J Thorac Oncol, 2018, 13(7):915-925

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Clin Cancer Res, 2018, 24(13):3097-3107

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Clin Cancer Res, 2018, 24(22):5610-5621

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Proc Natl Acad Sci U S A, 2018, 115(26):E6030-E6038

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Cancer Res, 2018, 10.1158/0008-5472.CAN-18-0505

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J Hematol Oncol, 2018, 11(1):109

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Sci Signal, 2018, 11(549)

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EBioMedicine, 2018, 29:112-127

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FASEB J, 2018, 10.1096/fj.201800011R

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Mol Cancer Ther, 2018, 17(4):740-750

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Mol Cancer Ther, 2018, 17(10):2257-2265

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Endocr Relat Cancer, 2018, 25(1):99-109

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Neoplasia, 2018, 20(8):826-837

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Nanomedicine (Lond), 2018, 13(10):1107-1120

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Lung Cancer, 2018, 126:72-79

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Front Cell Neurosci, 2018, 12:21

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Sci Rep, 2018, 8(1):18043

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Cancer Commun (Lond), 2018, 38(1):19

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Invest New Drugs, 2018, 36(6):999-1005

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Cancer Biol Ther, 2018, 19(3):239-247

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J Cancer Res Clin Oncol, 2018, 10.1007/s00432-018-2668-7

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Cancer Med, 2018, 7(1):208-218

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Oncol Rep, 2018, 40(2):1046-1054

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Environ Toxicol, 2018, 33(11):1153-1159

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Radiat Res, 2018, 189(3):283-291

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Pharmazie, 2018, 73(11):630-634

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Sci Rep, 2018, 8(1):14896

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JCI Insight, 2018, 3(24)

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JCI Insight, 2018, 3(11)

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Oncotarget, 2018, 9(101):37520-37533

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Oncotarget, 2018, 9(76):34240-34258

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Oncotarget, 2018, 9(51):29680-29697

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JCI Insight, 2018, 3(24)

PubMed: 30568033 ( click the link to review the publication )
Nanomedicine (Lond), 2018, 13(10):1107-1120

PubMed: 29874151 ( click the link to review the publication )

Oncotarget, 2018, 9(101):37520-37533

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Sci Transl Med, 2017, 9(415)

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Nat Commun, 2017, 8(1):410

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Nat Commun, 2017, 8:13897

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J Natl Cancer Inst, 2017, 1;109(9):djx014

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J Thorac Oncol, 2017, 12(5):884-889

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Clin Cancer Res, 2017, 23(12):3139-3149

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Genome Res, 2017, 27(4):613-625

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Genes Dev, 2017, 31(2):184-196

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Neuro Oncol, 2017, 19(12):1628-1639

PubMed: 28575494 ( click the link to review the publication )

Cancer Res, 2017, 77(11):2990-3000

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Cancer Res, 2017, 77(13):3527-3539

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Cancer Res, 2017, 10.1158/0008-5472

PubMed: 28202511 ( click the link to review the publication )

Cancer Res, 2017, 77(5):1200-1211

PubMed: 28082405 ( click the link to review the publication )

Cell Rep, 2017, 21(11):3298-3309

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Elife, 2017, 10.7554/eLife.21536

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J Med Chem, 2017, 60(17):7447-7458

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Arch Toxicol, 2017, 91(8):2921-2938

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Mol Cancer Ther, 2017,

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Mol Cancer Ther, 2017, 16(2):357-364

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Mol Cancer Ther, 2017, 16(10):2130-2143

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Mol Cancer Ther, 2017, 16(11):2563-2571

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Mol Cancer Ther, 2017, 16(3):506-515

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Mol Cancer Ther, 2017,

PubMed: 27913578 ( click the link to review the publication )

Mol Oncol, 2017,

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J Mol Biol, 2017, 429(14):2211-2230

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Eur J Med Chem, 2017, 140:510-527

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Transl Lung Cancer Res, 2017, 6(5):600-610

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Mol Cancer Res, 2017, 15(7):915-928

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Mol Cancer Res, 2017, 15(11):1542-1550

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Mol Cancer Res, 2017, 15(7):852-861

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Mol Pharm, 2017, 14(7):2368-2377

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Lung Cancer, 2017, 108:96-102

PubMed: 28625657 ( click the link to review the publication )

Lung Cancer, 2017, 109:1-8

PubMed: 28577937 ( click the link to review the publication )

Toxicol Sci, 2017, 162(1):146-166

PubMed: 29106658 ( click the link to review the publication )

Sci Rep, 2017, 7:44089

PubMed: 28276478 ( click the link to review the publication )

Clin Lung Cancer, 2017, 18(3):281-285

PubMed: 28038979 ( click the link to review the publication )

Toxicol Appl Pharmacol, 2017, 321:18-26

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Onco Targets Ther, 2017, 10:5281-5288

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Oncol Lett, 2017, 14(4):4349-4354

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J Vis Exp, 2017, (126)

PubMed: 28829429 ( click the link to review the publication )

Oncotarget, 2017, 8(62):105479-105491

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Oncotarget, 2017, 8(41):70736-70751

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Oncotarget, 2017, 9(2):1641-1655

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Oncotarget, 2017, 8(29):47305-47316

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Oncotarget, 2017, 8(55):93825-93838

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Oncotarget, 2017, 8(22):36331-36338

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Oncotarget, 2017, 8(65):109319-109331

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Oncotarget, 2017, 8(62):104894-104912

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Sci Rep, 2017, 7(1):15441

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Sci Rep, 2017, 7:44206

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Sci Rep, 2017, 7:44089

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Oncotarget, 2017, 9(2):1641-1655

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Mol Cell, 2016, 63(3):526-38

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Nat Commun, 2016, 7:11815

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Cancer Immunol Res, 2016, 4(11):936-947

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Oncogene, 2016, 10.1038/onc.2016.216

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J Med Chem, 2016, 59(13):6187-200

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Mol Cancer Ther, 2016, 15(12):3040-3054

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Cancer Sci, 2016, 107(8):1134-40

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Mol Pharm, 2016, 13(6):2117-25

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Oncotarget, 2016, 7(4):3847-56

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Oncotarget, 2016, 7(51):84951-84964

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Oncotarget, 2016, 7(30):47998-48010

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Oncotarget, 2016, 7(17):23608-32

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Sci Rep, 2016, 6:37997

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Oncotarget, 2016, 7(4):3847-56

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Clin Cancer Res, 2015, 21(23):5305-13

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Clin Cancer Res, 2015, 10.1158/1078-0432.CCR-15-0560

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Sci Signal, 2015, 8(379):ra53

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J Med Chem, 2015, 58(16):6589-606

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J Biol Chem, 2015, 290(28):17495-504

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PLoS One, 2015, 10(11):e0143333

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J Natl Compr Canc Netw, 2013, 11(10):1249-61

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Methods Mol Biol, 2011, 685:91-109

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Expert Opin Pharmacother, 2010, 11(8):1263-76

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Purity & Quality Control

Choose Selective EGFR Inhibitors

Biological Activity

Description

Features

Orally bioavailable mutant-selective EGFR inhibitor that has been tested in Phase III clinical trials for treatment of Non-Small Cell Lung Cancer.

Targets

L858R/T790M EGFR ^[1] (LoVo cells)	Exon 19 deletion EGFR ^[1] (LoVo cells)	WT EGFR ^[1] (LoVo cells)
11.44 nM	12.92 nM	493.8 nM

In vitro

AZD9291 shows significantly more potent inhibition of proliferation in mutant EGFR cell lines compared to wild-type in vitro. ^[2]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
PC-9/BRc1	NFjDdXhHfW6ldHnvckBCe3OjeR?=	NXrsXW4zPTBibl2=	MUGyOEBp	M1jNc2ROW09?	NVfPcmxmcW6mdXPld{BmgHC{ZYPzbY9vKG:oIITo[UBxem:jcH;weI91cWNiQlPMMVIh\mGvaXz5JI1mdWKncjDCTW0>	NG\yVlU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS3O\|MzPSd-MkW0O\|c{OjV:L3G+
PC-9/ERc1	NF;OR45HfW6ldHnvckBCe3OjeR?=	MmLxOVAhdk1?	MkTQNlQhcA>?	NHG5UXZFVVOR	MkXubY5lfWOnczDlfJBz\XO\|aX;uJI9nKHSqZTDwdo9ieG:ydH;0bYMhSkOOLUKg[oFucWy7IH3lcYJmeiCESV2=	NFPLNng9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS3O\|MzPSd-MkW0O\|c{OjV:L3G+
VP-2	NGrZR\|dHfW6ldHnvckBCe3OjeR?=	MV[1NEBvVQ>?	MlLJNlQhcA>?	NEP0RVZFVVOR	NUS2bGk1cW6mdXPld{BmgHC{ZYPzbY9vKG:oIITo[UBxem:jcH;weI91cWNiQlPMMVIh\mGvaXz5JI1mdWKncjDCTW0>	MlTHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2N{ezNlUoRjJ3NEe3N\|I2RC:jPh?=
PC-9/BRc1	M37KcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MX61NEBvVQ>?	MmG0NVAh\A>?	MV;EUXNQ	NVTMUHBrcW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBtd26pLYTldo0hMDFyLXThfUkh\3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYnz	MoLTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2N{ezNlUoRjJ3NEe3N\|I2RC:jPh?=
PC-9/ERc1	MlzPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NV7KW\|dVPTBibl2=	MkfYNVAh\A>?	MkjoSG1UVw>?	NGC5dI5qdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIxwdmdvdHXycUApOTBvZHH5LUBoem:5dHigbY5pcWKrdHnvckBie3OjeYO=	MlTqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2N{ezNlUoRjJ3NEe3N\|I2RC:jPh?=
VP-2	NIPSdJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MVO1NEBvVQ>?	NHL4eoMyOCCm	NE\3ZolFVVOR	NH3TPFBqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIxwdmdvdHXycUApOTBvZHH5LUBoem:5dHigbY5pcWKrdHnvckBie3OjeYO=	MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR5N{OyOUc,OjV2N{ezNlU9N2F-
PC9 GR4	NEjSfXZHfW6ldHnvckBCe3OjeR?=	MYiwMVExKM7:TR?=	M4DMSFczKGh?		M2fjdIlvcGmkaYTzxsBGT0[UIIDoc5NxcG:{eXzheIlwdiCjbnSg[I94dnO2cnXhcUB{cWewYXzpcofDqA>?	M162Z\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUS4OlM{Lz5{NUm0PFY{OzxxYU6=
PC9	M1HrbmZ2dmO2aX;uJGF{e2G7	MWCwMVExKM7:TR?=	NVjITFRiPzJiaB?=		M{GzOIlvcGmkaYTzJHdVKEWJRmKgZZQhdG:5IHPvcoNmdnS{YYTpc45{	MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl2OE[zN{c,OjV7NEi2N\|M9N2F-
PC9 GR4	M1;nb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MWSwMVExKM7:TR?=	MmezO\|IhcA>?		MoXibY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:\|ZTDk[ZBmdmSnboTsfS=>	Ml[4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7NEi2N\|MoRjJ3OUS4OlM{RC:jPh?=
BAF3	NXzHXI8yTnWwY4Tpc44h[XO\|YYm=		M3LvNVczKGh?		NU\ybHJxT0l3MDC9JFAvODByMzFOwG0>	NV3EZ5FERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyPFIyOjJpPkK4NlgzOTJ{PD;hQi=>
BAF3	NF7aclBHfW6ldHnvckBie3OjeR?=		MYm3NkBp		NYLl[lV1T0l3MDC9JFAvODByMzFOwG0>	MlTaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEKxNlIoRjJ6MkiyNVIzRC:jPh?=
BAF3	M4[ycmZ2dmO2aX;uJIF{e2G7		MUK3NkBp		NF\lUlVIUTVyIE2gNE4xODFizszN	NXL4PIc{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyPFIyOjJpPkK4NlgzOTJ{PD;hQi=>
HCC827	M2TNOmZ2dmO2aX;uJIF{e2G7		MWe3NkBp		M1jCN2dKPTBiPTCwMlAxOSEQvF2=	MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ6MkGyNkc,Ojh{OEKxNlI9N2F-
PC9	M{OwdWZ2dmO2aX;uJIF{e2G7		M1jZPVczKGh?		NWXiVnpuT0l3MDC9JFAvODB{IN88US=>	MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ6MkGyNkc,Ojh{OEKxNlI9N2F-
BAF3	NVLJPIhRTnWwY4Tpc44h[XO\|YYm=		MWq0JIg>		MV\FR\|UxKD1iMD6wNFIh\|ryP	MmfjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEKxNlIoRjJ6MkiyNVIzRC:jPh?=
HCC827	M2rucGZ2dmO2aX;uJIF{e2G7		NUXNZY91OyCq		NFPG[\|hKSzVyIE2gNE4xODJ3IN88US=>	MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzR\|M{iyPUc,Ojd2M{O4Nlk9N2F-
H1975	Mn\YSpVv[3Srb36gZZN{[Xl?		NU\SfnV1OyCq		NY[4T\|Y3UUN3MDC9JFAvODB{NTFOwG0>	NWq4foNPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke0N\|M5OjlpPkK3OFM{QDJ7PD;hQi=>
H3255	MUjGeY5kfGmxbjDhd5NigQ>?		M3\YUFMhcA>?		M1\xbmlEPTBiPTCwMlAxPDFizszN	MlfkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd2M{O4NlkoRjJ5NEOzPFI6RC:jPh?=
NCI-H1975	NWHr[3NPTnWwY4Tpc44h[XO\|YYm=		MVy3NkBp		NWHQ[pNFT0l3MDC9JFAvODB3IN88US=>	Mor1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEKxNlIoRjJ6MkiyNVIzRC:jPh?=
PC9	MWnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>?		MUC3NkBp		M3znUWlEPTBiPTCwMlAxPjVizszN	NFzaSZc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEexOlY1OSd-Mki3NVY3PDF:L3G+
NCI-H1975	M4PDPWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7		M1PlfFczKGh?		NFvCWVVKSzVyIE2gNE4xOTB3IN88US=>	NWKzS5U4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki3NVY3PDFpPkK4O\|E3PjRzPD;hQi=>
Sf21	MkPuSpVv[3Srb36gZZN{[Xl?				M3rMR2lEPTBiPTCwMlAyOiEQvF2=	Mlq4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7OU[yOlcoRjJ5OUm2NlY4RC:jPh?=
PC9-DRH	M3e3TWZ2dmO2aX;uJIF{e2G7		NVjmOZR7OiCq		NInhZYFKSzVyIE2gNE4xOTNizszN	M2L1elxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4N{W2NlIzLz5{Nke1OlIzOjxxYU6=
BAF3	MXXGeY5kfGmxbjDhd5NigQ>?		NVPNWIg{PzJiaB?=		MlHZS2k2OCB;IECuNFE{KM7:TR?=	M1TpclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkiyNVIzLz5{OEK4NlEzOjxxYU6=
HCC827	M331UWZ2dmO2aX;uJIF{e2G7		MkPRPVYhcA>?		NUizRmdiTUN3MDC9JFAvODF2IN88US=>	NEfW[2w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEKyOVI3QSd-MkiyNlUzPjl:L3G+
HCC827	M3T6fGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7		NFnlUFA6PiCq		M3q1XGVEPTBiPTCwMlAyPCEQvF2=	M4r4XVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OEWzOVc2Lz5{OEi1N\|U4PTxxYU6=
NCI-H1975	MVnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>?		M1nVdFk3KGh?		NGfie5VGSzVyIE2gNE4xOTRizszN	MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDh3M{W3OUc,Ojh6NUO1O\|U9N2F-
NCI-H1975	NVvDZYFTTnWwY4Tpc44h[XO\|YYm=		NF3OSGIzKGh?		MmPWTWM2OCB;IECuNFE2KM7:TR?=	NUfMO2RbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[3OVYzOjJpPkK2O\|U3OjJ{PD;hQi=>
H1975	NInNT4dHfW6ldHnvckBie3OjeR?=		M4ewVVIhcA>?		M2jpdmlEPTBiPTCwMlAyPSEQvF2=	MlrrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ7NkiyOVMoRjJ4OU[4NlU{RC:jPh?=
PC9	NYmwZZNxTnWwY4Tpc44h[XO\|YYm=		M4i0V\|IhcA>?		MUTJR\|UxKD1iMD6wNVch\|ryP	NGPEUHc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nkm2PFI2Oyd-Mk[5OlgzPTN:L3G+
NCI-H1975	NHjrOYlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?=		Mnq5O\|IhcA>?		NFH6SYNKSzVyIE2gNE4xOTlizszN	NGrYb2Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUS2Olc4Oyd-Mkm0OlY4PzN:L3G+
NCI-H1975	NGC3TVJHfW6ldHnvckBie3OjeR?=		MYG5OkBp		MlfRSWM2OCB;IECuNFE6KM7:TR?=	NGDjOng9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEKyOVI3QSd-MkiyNlUzPjl:L3G+
NCI-H1975	MlzHRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl?		NHPYNW86PiCq		MoqwSWM2OCB;IECuNFE6KM7:TR?=	MkfJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh4MEO5PVEoRjJ6NkCzPVkyRC:jPh?=
NCI-H1975	NYXE[Gl5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO\|YYm=		Mnq3O\|IhcA>?		Mo[zTWM2OCB;IECuNFE6KM7:TR?=	NH;hU4M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUi1N\|M1OCd-Mkm4OVM{PDB:L3G+
HCC827	NHvT[VFHfW6ldHnvckBie3OjeR?=		M2LkXFIhcA>?		MVvJR\|UxKD1iMD6wNlMh\|ryP	NXnCdlFNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[3OVYzOjJpPkK2O\|U3OjJ{PD;hQi=>
NCI-H1975	NHe0OXJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?=		Mo[wO\|IhcA>?		NUDyWpdqUUN3MDC9JFAvODJ\|IN88US=>	MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV\|NEmyOkc,Ojl3M{S5NlY9N2F-
PC9	NUHkXZVlS3m2b4TvfIlkcXS7IHHzd4F6		M2juSVczKGh?		MmPLS2k2OCB;IECuNFI{KM7:TR?=	NYDmN\|J3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyO\|E6PjNpPkK1NlcyQTZ\|PD;hQi=>
NCI-H1975	M4TMSmN6fG:2b4jpZ4l1gSCjc4PhfS=>		M4H1elczKGh?		MkjZS2k2OCB;IECuNFI1KM7:TR?=	NXXVU4JXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyO\|E6PjNpPkK1NlcyQTZ\|PD;hQi=>
HCC827	MXPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>?		M2f1OlczKGh?		NVmxVWVUUUN3MDC9JFAvODJ3NDFOwG0>	M17PVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUe2NlczLz5{OUW3OlI4OjxxYU6=
HCC827	MkLjRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl?		MoXlO\|IhcA>?		NYfjTm5OUUN3MDC9JFAvODJ5IN88US=>	Mn7DQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2Nk[3O\|MoRjJ7NE[2O\|c{RC:jPh?=
HCC827	MmPFRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl?		M2LqNVczKGh?		MmHMTWM2OCB;IECuNFI4KM7:TR?=	MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTh3M{O0NEc,Ojl6NUOzOFA9N2F-
NCI-H1975	MWrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>?		MXG3NkBp		NVO2ZocxUUN3MDC9JFAvODNizszN	MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDB\|M{W3PUc,OjhyM{O1O\|k9N2F-
H3255	MkTYSpVv[3Srb36gZZN{[Xl?		MXu3NkBp		NWS3SWhrT0l3MDC9JFAvODN\|IN88US=>	NGGzSVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NlEzOid-MkiyPFIyOjJ:L3G+
H3255	NUn3bmpuTnWwY4Tpc44h[XO\|YYm=		M1j3cVIhcA>?		NHLVdpFKSzVyIE2gNE4xOzZizszN	NF;xXYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nke1OlIzOid-Mk[3OVYzOjJ:L3G+
NCI-H1975	MV7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>?		MnPkO\|IhcA>?		M1XPemlEPTBiPTCwMlA1OSEQvF2=	NFXOe3Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUezNFE6Oid-Mkm3N\|AyQTJ:L3G+
NCI-H1975	NUDXZ\|JSTnWwY4Tpc44h[XO\|YYm=		NEeyVG4yKGh?		M1rSVWlEPTBiPTCwMlA1OSEQvF2=	NIGwUmw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWzOFkzPid-Mkm1N\|Q6OjZ:L3G+
BAF3	NGTQdo9HfW6ldHnvckBie3OjeR?=		M4DPVFQhcA>?		MVzFR\|UxKD1iMD6wOFMh\|ryP	NIDGe3A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NlEzOid-MkiyPFIyOjJ:L3G+
NCI-H1975	MlfyRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl?		MnnLO\|IhcA>?		NGHKd3FKSzVyIE2gNE4xPDd{IN88US=>	NETEOYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUW3OlI4Oid-Mkm1O\|YzPzJ:L3G+
NCI-H1975	NXTxd2puSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO\|YYm=		NITNdYs4OiCq		MlfITWM2OCB;IECuNFUzKM7:TR?=	M3fvNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUOxOlM6Lz5{N{GzNVY{QTxxYU6=
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rat hepatocytes	NITxTFdHfW6ldHnvckBie3OjeR?=				M1n4XWlvfHKrboPpZ{BkdGWjcnHuZ4UhcW5icnH0JIhmeGG2b3P5eIV{KG2nYYP1doVlKHCncjCxNEc3KGOnbHzz	MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ5MUm2N{c,OjV{N{G5OlM9N2F-
human hepatocytes	NXTlS3pHTnWwY4Tpc44h[XO\|YYm=				M2D6W2lvfHKrboPpZ{BkdGWjcnHuZ4UhcW5iaIXtZY4hcGWyYYTvZ5l1\XNibXXhd5Vz\WRicHXyJFExLzZiY3XscJM>	NITSfHI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK3NVk3Oyd-MkWyO\|E6PjN:L3G+
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A431	M1XHTGZ2dmO2aX;uJIF{e2G7				NETxOHdU\WynY4Tpeol1gSC{YYTpc{Bw\iCHQ{WwJIZweiCqdX3hckBCPDNzIHPlcIx{KGW6cILld5Nqdmdid3ns[EB1gXCnIFXHSnIhfG9iRVO1NEBnd3JiaIXtZY4hVkOLLVixPVc2KGOnbHzzJIhiemKxcnnu[{BGT0[ULVy4OVhTN1R5OUDNJIRwfWKuZTDteZRidnR?	M363NlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OEWzOVc2Lz5{OEi1N\|U4PTxxYU6=
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Caco2	M2P2SmZ2dmO2aX;uJIF{e2G7		M1zRNlIhcA>?		MX3BdJBiemWwdDDw[ZJu\WGkaXzpeJkh[WO{b4PzJIJie2:uYYTldoFtKHSxIHHwbYNidCC\|aXTlJIlvKGi3bXHuJGNi[29{IHPlcIx{KGG2IEWgeW0hcW6ldXLheIVlKG[xcjCyJIhzew>?	MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDh3M{W3OUc,Ojh6NUO1O\|U9N2F-
NCI-H1975	NGjpRYlHfW6ldHnvckBie3OjeR?=		MYK0JIg>		Mk\XTY5pcWKrdHnvckBw\iCHR1\SJGw5PTiUL2S3PVBOKG23dHHueEBqdiCqdX3hckBPS0lvSEG5O\|Uh[2WubIOgZZN{\XO\|ZXSgZZMhemWmdXP0bY9vKGmwIFHreEBxcG:\|cHjvdplt[XSrb36gZZQhXGi{M{C4M3NmejR5MzDzbZRmKGG2IEGgeW0hdWWjc4Xy[YQh[W[2ZYKgOEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{	M37CRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkiyNVIzLz5{OEK4NlEzOjxxYU6=
HCC827	NHrjRpFHfW6ldHnvckBie3OjeR?=		MlfiOEBp		MmHiTY5pcWKrdHnvckBw\iCHR1\SJIV5d25iMUmg[IVt\XSrb36gcZV1[W62IHnuJIh2dWGwIFjDR\|gzPyClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gRYt1KHCqb4PwbI9zgWyjdHnvckBifCCWaIKzNFgwW2W{NEezJJNqfGViYYSgNUB2VSCvZXHzeZJm\CCjZoTldkA1KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN?	MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ6MkGyNkc,Ojh{OEKxNlI9N2F-
NCI-H1975	NWn4[Hh2SXCxcITvd4l{KGG\|c3H5		Ml3EOFghcA>?		MWHJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKE6FST3INVk4PSClZXzsd{Bp[XKkb4LpcochTUeIUjDMPFU5Wi:WN{mwUUBufXSjboSgZZN{\XO\|ZXSgZZMh[2G\|cHHz[VMh[2ynYY\h[4Uh[XRiMTD1UUBi\nSncjC0PEBpenNiYomgbY1ufW6xYnzveJRqdmd?	M1PVO\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkiyNVIzLz5{OEK4NlEzOjxxYU6=
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HCC827	MX3BdI9xfG:\|aYOgZZN{[Xl?		MUm0PEBp		NHXBU2NKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m\|IHnuJIh2dWGwIFjDR\|gzPyClZXzsd{Bp[XKkb4LpcochTUeIUjDlfI9vKDF7IHTlcIV1cW:wIH31eIFvfCCjc4Pld5Nm\CCjczDQRXJRKGOuZXH2ZYdmKGG2IEGgeW0h[W[2ZYKgOFghcHK\|IHL5JIludXWwb3Lsc5R1cW6p	NInhS5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NlEzOid-MkiyPFIyOjJ:L3G+
H3255	NWXXNFcySXCxcITvd4l{KGG\|c3H5		MUW0PEBp		M17qWGlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iSEOyOVUh[2WubIOgbIFz[m:{aX7nJGVITlJiTEi1PHIhdXW2YX70JIF{e2W\|c3XkJIF{KFCDUmCgZ4xm[X[jZ3WgZZQhOSC3TTDh[pRmeiB2ODDodpMh[nliaX3teY5w[myxdITpcoc>	NHjCVZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NlEzOid-MkiyPFIyOjJ:L3G+
NCI-H1975	M2PLcWZ2dmO2aX;uJIF{e2G7				MYTT[Yxm[3Srdnn0fUBz[XSrbzDv[kBKSzVyIH\vdkBpfW2jbjDOR2kuUDF7N{WgZ4VtdHNiaHHyZo9zcW6pIFXHSnIhVDh3OGKvWFc6OE1iZH;1ZoxmKG23dHHueEB1dyCLQ{WwJIZweiCqdX3hckBCPDNzIHPlcIx{KGijcnLvdolv\yC5aXzkMZR6eGViRVfGVi=>	M2HWRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NEK2PVk3Lz5{OESyOlk6PjxxYU6=
human hepatocytes	M4W5cmZ2dmO2aX;uJIF{e2G7				Ml\PTY51emmwc3njJINt\WG{YX7j[UBqdiCqdX3hckBp\XCjdH;jfZRmeyCjc4Pld5Nm\CCyZYKgcYltdGmxbjDj[Yxtew>?	NX;LZVJuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0NlY6QTZpPkK4OFI3QTl4PD;hQi=>
rat hepatocytes	NXT6XYpzTnWwY4Tpc44h[XO\|YYm=				M1q4OWlvfHKrboPpZ{BkdGWjcnHuZ4UhcW5icnH0JIhmeGG2b3P5eIV{KGG\|c3Xzd4VlKHCncjDtbYxtcW:wIHPlcIx{	M1zUXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NEK2PVk3Lz5{OESyOlk6PjxxYU6=
A549, NCI-H1975	MYfGeY5kfGmxbjDhd5NigQ>?				MXTT[Yxm[3Srdnn0fUBz[XSrbzDv[kBKSzVyIH\vdkBGT0Zvc4TpcZVt[XSnZDD3bYxlKHS7cHWgSWdHWiCrbjDoeY1idiCDNUS5JINmdGy\|IITvJGlEPTBiZn;yJGVITlJiTEi1PHIwXDd7MF2g[I92[mynIH31eIFvfCCrbjDoeY1idiCQQ1mtTFE6PzViY3XscJM>	NETodVg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nke1OlIzOid-Mk[3OVYzOjJ:L3G+
A549, PC9	MYDGeY5kfGmxbjDhd5NigQ>?				MmT2V4Vt\WO2aY\peJkhemG2aX:gc4YhUUN3MDDmc5IhTUeILYP0bY12dGG2ZXSge4lt\CC2eYDlJGVITlJiaX6gbJVu[W5iQUW0PUBk\WyuczD0c{BKSzVyIH\vdkBGT0[UIHTlcIV1cW:wIH31eIFvfCCrbjDoeY1idiCSQ{mgZ4VtdHN?	M4HKbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4N{W2NlIzLz5{Nke1OlIzOjxxYU6=
HCC827	Mn7uRZBweHSxc3nzJIF{e2G7				M2rnOmlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iSFPDPFI4KGOnbHzzJIhiemKxcnnu[{BGT0[UIFW3OFYhfG9iQUe1NEBl\WyndHnvckBufXSjboSgZZN{\XO\|ZXSgZZMh\WG{bImgZZBweHSxdHnjJINmdGy\|IHH0JFMhfU1iYX\0[ZIhOjRiaILzJIJ6KEGwbnX4bY4hXi2ISWTDM5Bzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnegZoF{\WRiZnzve{BkgXSxbXX0dpkhMFK4YjC9JFEvOzRidH:gNU43PyVr	NHTaSnE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUi1N\|M1OCd-Mkm4OVM{PDB:L3G+
NCI-H1975	M1L5UmZ2dmO2aX;uJIF{e2G7				NUnmWXljUW6qaXLpeIlwdiCxZjDFS2ZTKEx6NUjSM3Q4QTCPIHTveYJt\SCvdYThcpQheGixc4Doc5J6dGG2aX;uJIlvKEWJRj3zeIlufWyjdHXkJIh2dWGwIF7DTU1JOTl5NTDj[YxteyCjdDCxJJRwKDFyMDDuUUBjgSCZZYP0[ZJvKGKub4SgcYV1cG:m	M17qU\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OUC2NVE1Lz5{OUmwOlEyPDxxYU6=
A431	NYDUV4hJTnWwY4Tpc44h[XO\|YYm=				MnHvV4Vt\WO2aY\peJkhemG2aX:sJJJifGmxIFnDOVAh\m:{IHj1cYFvKEF2M{GgZ4VtdHNib4\ldoV5eHKnc4Ppcochf2muZD30fZBmKEWJRmKgeI8hUUN3MDDmc5IhcHWvYX6gUmNKNUhzOUe1JINmdGy\|IHX4dJJme3OrbnegSWdHWiCWN{mwUU9NQDV6UjDteZRidnR?	NFTuS5c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{GzNVY{QSd-MkexN\|E3Ozl:L3G+
PC9	MlG2RY51cXS3bX;yJIFkfGm4aYT5JIF{e2G7				MUHBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCSQ{mgZ4VtdHNiaHHyZo9zcW6pIFXHSnIh\XixbjCxPUBl\WyndHnvckBi[3SrdnH0bY5oKG23dHHueEB5\W6xZ4Lh[pRm\CCrbjDTR2lFKG2xdYPlJIF{e2W\|c3XkJIF{KHS3bX;yJIdzd3e2aDDpcohq[mm2aX;uJIF1KDFyIH3nM4toN2SjeTygdI8heWRiZn;yJFch\GG7czDy[YxifGm4ZTD0c{Bkd262cn;s	MmCzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{N{G5OlMoRjJ3MkexPVY{RC:jPh?=
A431	MmjpRY51cXS3bX;yJIFkfGm4aYT5JIF{e2G7				NFTSdGZCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOFMyKGOnbHzzJJhmdm:pcnHmeIVlKGmwIGPDTWQhdW:3c3WgZZN{\XO\|ZXSgZZMhfHWvb4Kg[5Jwf3SqIHnubIljcXSrb36gZZQhPSCvZz;r[{9l[XluIIDvJJFlKG[xcjC3JIRigXNicnXsZZRqfmVidH:gZ49vfHKxbB?=	NH3sSVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK3NVk3Oyd-MkWyO\|E6PjN:L3G+

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p-EGFR / p-AKT / p-ERK; PubMed: 28416483 Cancer Res PC-9/BRc1 cells were treated with the indicated doses of osimertinib. Drugs were refreshed every 24 hours. Cellular lysates were probed with the indicated antibodies. Osim: osimertinib. ABCB1; PubMed: 27649127 Molecules The effect of osimertinib at 0.3 μM on the expression of ABCB1 was measured in KB-3-1 and KB-C2 cell lines for 0, 24, 48, and 72 h.	28416483 27649127
Growth inhibition assay	Cell viability; PubMed: 31043587 Cell Death Dis Cells were treated with gefitinib or osimertinib for 72 h. Cell viability was measured by MTT assay. P < 0.05, P < 0.01, **P < 0.005 by t-test.	31043587
Immunofluorescence	Ki67 / γH2AX / p16; PubMed: 29212784 EMBO Mol Med PC9ER cells were treated for 5 days with either 3×mAbs (20 μg/ml), saline (CTRL), or with a low dose of osimertinib (2.5 nM). Shown are representative images of cells fixed in paraformaldehyde and immunostained for KI67 (panel E), γH2AX (panel F), and p16 (panel G). DAPI counterstaining was used to follow nuclear localization. Scale bar, 20 μm. The box and whisker plots, where the ends of the box are the upper and lower quartiles, depict quantifications of results obtained in three independent experiments. P ≤ 0.01, *P ≤ 0.001, n = 4; one-way ANOVA with Tukey's test.	29212784

In vivo

AZD9291(5mg/kg p.o.) causes profound regression of tumors across EGFRm+ (PC9) and EGFRm+/T790M (H1975) tumor models with profound inhibition of EGFR phosphorylation and key downstream signaling pathways such as AKT and ERK in vivo. ^[2]

Protocol

Animal Research: ^[2]	- Collapse Animal Models: Mice bearing PC9 and H1975 xenograft tumors Dosages: ~5 mg/kg Administration: p.o. (Only for Reference)

References

Solubility (25°C)

In vitro	DMSO	99 mg/mL warmed (198.15 mM)
	Water	Insoluble
	Ethanol	'43 mg/mL warmed
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 5%DMSO+40%PEG300+5%Tween80+50%ddH2O For best results, use promptly after mixing.	7.5mg/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 Osimertinib (AZD9291) SDF

Molecular Weight	499.61
Formula	C₂₈ H₃₃ N₇ O₂
CAS No.	1421373-65-0
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	Mereletinib
Smiles	CN1C=C(C2=CC=CC=C21)C3=NC(=NC=C3)NC4=C(C=C(C(=C4)NC(=O)C=C)N(C)CCN(C)C)OC

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

% DMSO+ % + % Tween 80+ % ddH₂O

Calculate Reset

Calculation results:

Working concentration： mg/ml；

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 μL 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.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Bio Calculators

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2021-01-06)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02841579	Completed	Drug: Osimertinib	Non-Small Cell Lung Cancer	MedSIR\|AstraZeneca	August 2016	Phase 2
NCT02771314	Active not recruiting	Drug: AZD9291	Non Small Cell Lung Cancer	Hellenic Oncology Research Group	August 2 2016	Phase 2
NCT02511106	Active not recruiting	Drug: AZD9291 80 mg/40 mg\|Drug: Placebo AZD9291 80 mg/40 mg	Stage IB-IIIA Non-small Cell Lung Carcinoma	AstraZeneca	October 21 2015	Phase 3
NCT02529995	Completed	Drug: AZD9291 40 mg\|Drug: AZD9291 80 mg	Carcinoma Non-Small-Cell Lung With EGFR Mutation Positive	AstraZeneca	August 24 2015	Phase 1
NCT02491944	Completed	Drug: AZD9291\|Drug: [14C]AZD9291	Oncology	AstraZeneca	July 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

If you have any other enquiries, please leave a message.

Frequently Asked Questions

Question 1:
Can this formulation be used in mice? What are reconstitution instructions for in vivo with mice?
Answer:
Osimertinib can be used for animal study. The vehicle we suggest is: 1% DMSO+30% PEG 300+dd H2O at up to 30mg/ml.

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