Gefitinib (ZD1839)

Name: Gefitinib (ZD1839)
Brand: Selleck Chemicals
SKU: S1025
Rating: 5 (479 reviews)

For research use only.

Catalog No.S1025 Synonyms: Iressa

479 publications

CAS No. 184475-35-2

Gefitinib (ZD-1839, Iressa) is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively. Gefitinib promotes autophagy and apoptosis of lung cancer cells via blockade of the PI3K/AKT/mTOR pathway.

Selleck's Gefitinib (ZD1839) has been cited by 479 publications

Cell Stem Cell, 2020, 7;26(5):782-792e7

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Cancer Cell, 2020, 13;37(1):104-122e12

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Cancer Discov, 2019, 9(7):926-943

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Cell Stem Cell, 2019, 25(1):69-86

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Cell, 2018, 172(1-2):373-386

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Nat Med, 2018, 24(4):512-517

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Nat Methods, 2018, 15(8):631-639

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Cancer Cell, 2018, 34(3):427-438

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Nature, 2017, 547(7664):453-457

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Nature, 2016, 30;534(7609):647-51.

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Nat Med, 2016, 22(3):262-9

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Cancer Discov, 2015, 5(7):713-22

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Cancer Discov, 2015, 5(9):960-971

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Nature, 2014, 3;508(7494):118-22.

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Nat Med, 2013, 19(11):1469-1472

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Nature, 2012, 26;483(7387):100-3.

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Cell, 2012, 21;151(5):937-50.

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Cancer Discov, 2012, 2(10):934-47

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Cancer Discov, 2011, 1(7):608-25

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Theranostics, 2021, 11(2):824-840

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Theranostics, 2021, 11(6):2594-2611

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Mol Cancer, 2021, 20(1):17

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Cancers (Basel), 2021, 13(2)E272

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PLoS Pathog, 2021, 17(1):e1009221

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Cell Death Dis, 2021, 12(1):83

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Drug Metab Dispos, 2021, 49(1):53-61

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Acta Neuropathol, 2020, 17

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Acta Neuropathol, 2020, 10.1007/s00401-020-02226-7

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Nat Commun, 2020, 21;11(1):1923

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Nat Commun, 2020, 11(1):4607

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Nat Commun, 2020, 25;11(1):1556

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Sci Adv, 2020, 6(11):eaax2271

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EMBO Mol Med, 2020, 12(8):e11987

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Clin Cancer Res, 2020, clincanres.3555.2020

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Clin Cancer Res, 2020, 10.1158/1078-0432

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Mol Syst Biol, 2020, 16(2):e8664

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Cancer Res, 2020, 80(22):4998-5010

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Aging Cell, 2020, 22:e13145

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Elife, 2020, 9e60541

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Redox Biol, 2020, 38:101780

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Oncogene, 2020, 10.1038/s41388-020-01465-y

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

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Cancer Lett, 2020, 475:109-118

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Sci Signal, 2020, 3;13(621) pii: eaax2364

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Cancers (Basel), 2020, 12(12)E3761

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Cancers (Basel), 2020, 27;12(5)pii: E1087

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Cancers (Basel), 2020, 13;12(2) pii: E436

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Cancers (Basel), 2020, 12(2)

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Cancers (Basel), 2020, 12(2)

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Cell Death Dis, 2020, 11(9):768

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Cell Death Dis, 2020, 11(2):143

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Br J Cancer, 2020, 10.1038/s41416-020-0952-1

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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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Front Immunol, 2020, 10:3135

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Mol Cancer Ther, 2020, 5 pii: molcanther

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Mol Cell Proteomics, 2020, 31 pii: mcp

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Neurobiol Dis, 2020, 9;104961

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J Cancer, 2020, 6;11(13):3762-3770

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Transl Lung Cancer Res, 2020, 9(5):1904-1914

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Cancer Sci, 2020, 111(5):1652-1662

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

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Am J Cancer Res, 2020, 10(12):4251-4265

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Oncogenesis, 2020, 9(10):87

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Biomolecules, 2020, 10(1)

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Mol Cancer Res, 2020, 10.1158/1541-7786.MCR-19-0669

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Mol Cancer Res, 2020, 25

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Front Oncol, 2020, 9:1503

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Front Oncol, 2020, 12;10:696

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Front Oncol, 2020, 10:554704

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Cell Microbiol, 2020, e13240

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J Cell Mol Med, 2020, 24(10):5578-5592

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J Cell Mol Med, 2020, 24(10):5811-5816

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Int J Mol Sci, 2020,

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Int J Mol Sci, 2020, 21(20)E7770

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Sci Rep, 2020, 10(1):17768

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

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Cancer Cell Int, 2020, 19;20:58

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Biomed Pharmacother, 2020, 16;127:110225

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Invest New Drugs, 2020, 38(4):1003-1011

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Am J Transl Res, 2020, 12(11):7377-7385

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Infect Immun, 2020, 88(4)e00819-19

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Oncol Rep, 2020, 45(2):459-468

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Eur J Pharmacol, 2020, 5;874:172961

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J Pharm Biomed Anal, 2020, 195:113864

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Thorac Cancer, 2020, 5

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Thorac Cancer, 2020, 10.1111/1759-7714.13533

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Thorac Cancer, 2020, 10.1111/1759-7714.13670

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Hum Cell, 2020, 10.1007/s13577-020-00425-8

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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 Thorac Dis, 2020, 12(3):712-723

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Int J Radiat Biol, 2020, 96(4):461-468

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Cold Spring Harb Mol Case Stud, 2020,

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Cell Death Dis, 2020, 11(8):670

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Fundam Clin Pharmacol, 2020, 10.1111/fcp.12641

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BMC Cancer, 2020, 20(1):1189

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Exp Mol Med, 2020, 10.1038/s12276-020-0474-1

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Cells, 2020, 9(8):E1830

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Cytometry A, 2020, 97(1):70-77

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Redox Biol, 2020, 36:101652

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Cell Rep, 2020, 32(5):107994

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Viruses, 2020, 12(11)E1294

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Exp Cell Res, 2020, 390(2):111950

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Cell Syst, 2020, S2405-4712(20)30247-7

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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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Cancer Treat Res Commun, 2020, 25:100229

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Exp Ther Med, 2020, 20(2):1415-1422

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Nat Cell Biol, 2019, 21(6):778-790

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Mol Cell, 2019, 73(1):166-182

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Hepatology, 2019, 10.1002/hep.30780

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Nat Commun, 2019, 10(1):2701

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Nano Lett, 2019, 19(10):7526-7533

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Nat Commun, 2019, 10(1):2919

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Autophagy, 2019, 10.1080/15548627.2019.1660545

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EMBO J, 2019, 38(4)

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Cancer Res, 2019, 79(4):819-829

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J Am Soc Nephrol, 2019, 30(8):1454-1470

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Matrix Biol, 2019, 10.1016/j.matbio.2019.07.006

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Cell Rep, 2019, 26(1):65-78

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Mol Cancer, 2019,

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Elife, 2019,

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Int J Cancer, 2019, 10.1002/ijc.32487

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

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Oncogene, 2019, 38(14):2464-2481

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Oncogene, 2019, 38(11):1936-1950

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

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J Exp Clin Cancer Res, 2019, 38(1):46

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J Exp Clin Cancer Res, 2019, 38(1):96

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

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Cancers (Basel), 2019, 11(1)

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Cancers (Basel), 2019, 11(10)

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Breast Cancer Res, 2019, 21(1):77

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Cell Death Dis, 2019, 10(4):283

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Signal Transduct Target Ther, 2019,

PubMed: 32651361 ( click the link to review the publication )

Signal Transduct Target Ther, 2019, 4:25

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Cells, 2019, 8(12)

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Cells, 2019, 8(12)E1495

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Cell Physiol Biochem, 2019, 53(5):805-819

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Mol Cancer Ther, 2019, 10.1158/1535-7163.MCT-19-0181

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Cell Prolif, 2019, 52(6):e12680

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Cell Prolif, 2019,

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Neoplasia, 2019, 22(1):1-9

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Biomolecules, 2019, 9(10)E638

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Lung Cancer, 2019, 137:85-93

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Cancer Biol Med, 2019, 16(3):606-617

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Artif Cells Nanomed Biotechnol, 2019, 47(1):3231-3238

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DNA Repair (Amst), 2019, 78:37-44

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Front Oncol, 2019, 9:1167

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

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Biochem Pharmacol, 2019, 169:113640

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Int J Mol Sci, 2019, 20(19)

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Sci Rep, 2019, 9(1):1897

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Sci Rep, 2019,

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J Biol Chem, 2019, 294(12):4488-4497

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Mol Pharmacol, 2019, 95(5):528-536

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Cancer Cell Int, 2019, 19:117

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Mol Carcinog, 2019, 10.1002/mc.23139

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Mol Carcinog, 2019,

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Front Pharmacol, 2019, 10:1116

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Respir Res, 2019, 20(1-:270

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Respir Res, 2019, 20(1):164

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Biomed Pharmacother, 2019, 118:109169

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J Proteomics, 2019, 195:114-124

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Int J Mol Sci, 2019, 20(10)

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Int J Oncol, 2019, 54(2):527-536

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Mediators Inflamm, 2019,

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Life Sci, 2019, 224:23-32

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J Drug Target, 2019, 27(4):451-459

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Int J Biochem Cell Biol, 2019, 106:96-106

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Molecules, 2019, 24(3)

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Transl Oncol, 2019, 12(11):1516-1524

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Eur J Pharmacol, 2019, 855:10-19

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Eur J Pharmacol, 2019, 850:97-108

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Eur J Pharmacol, 2019, 856:172409

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Biosci Rep, 2019, 39(8)

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PLoS ONE, 2019,

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Onco Targets Ther, 2019, 12:6033-6043

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Biomed Res Int, 2019, 2019:3129748

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J Cancer Prev, 2019, 24(4):217-223

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Mol Med Rep, 2019,

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Oncol Lett, 2019, 18(5):5621-5627

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Oncol Lett, 2019, 18(1):368-374

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Anticancer Res, 2019, 39(7):3785-3793

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Clin Respir J, 2019, 13(1):23-33

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Exp Ther Med, 2019, 18(5):3793-3800

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Exp Ther Med, 2019, 17(1):953-959

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Cancer Immunol Res, 2019,

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Zhongguo Fei Ai Za Zhi, 2019, 22(5):255-263

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

PubMed: 31108249 ( click the link to review the publication )

Oncotarget, 2019, 10(11):1171-1192

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Nat Microbiol, 2019, 4(2):216-225

PubMed: 30420785 ( click the link to review the publication )

JCI Insight, 2019, 4(21)

PubMed: 31600169 ( click the link to review the publication )

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

PubMed: 31069016 ( click the link to review the publication )

Nat Biomed Eng, 2018, 2(8):578-588

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

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Nat Commun, 2018, 9(1):4728

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Nat Commun, 2018, 9(1):2434

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EMBO Mol Med, 2018, 10(3)

PubMed: 29449326 ( click the link to review the publication )

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

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Clin Cancer Res, 2018, 24(16):3928-3940

PubMed: 29685880 ( click the link to review the publication )

EMBO Rep, 2018,

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Theranostics, 2018, 8(5):1256-1269

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J Control Release, 2018, 275:117-128

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

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Oncogene, 2018, 37(12):1576-1593

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Oncogene, 2018, 37(9):1251-1262

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Cancer Lett, 2018, 424:84-96

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Sci Signal, 2018, 11(549)

PubMed: 30254057 ( click the link to review the publication )

J Exp Clin Cancer Res, 2018, 3;37(1):131

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Cancers (Basel), 2018, 10(6)

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FASEB J, 2018, 10.1096/fj.201800011R

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Exp Mol Med, 2018, 50(1):e435

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Exp Mol Med, 2018, 50(4):52

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Cell Physiol Biochem, 2018,

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Cell Physiol Biochem, 2018, 51(1):337-355

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Endocr Relat Cancer, 2018, 25(4):471-480

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Cell Commun Signal, 2018, 16(1):77

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Mol Oncol, 2018,

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Mol Oncol, 2018, 12(6):883-895

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Mol Oncol, 2018, 12(2):224-238

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Mol Cell Proteomics, 2018, 17(10):1892-1908

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Eur J Med Chem, 2018, 144:330-348

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Cancer Sci, 2018, 109(6):1775-1786

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Oncogenesis, 2018, 7(9):67

PubMed: 30190455 ( click the link to review the publication )

Mol Cancer Res, 2018, 16(3):543-553

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Mol Cancer Res, 2018, 16(10):1458-1469

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Mol Cancer Res, 2018, 16(11):1773-1784

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Mol Cancer Res, 2018, 16(7):1185-1195

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J Immunol, 2018, 200(8):2809-2818

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J Cell Sci, 2018,

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Antiviral Res, 2018, 150:20-29

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Biochem Pharmacol, 2018, 152:327-337

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Sci Rep, 2018, 8(1):18043

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J Biol Chem, 2018, 293(35):13401-13414

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Respir Res, 2018, 19(1):96

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Cancer Manag Res, 2018, 10:5785-5798

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Cancer Manag Res, 2018, 10:6695-6703

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Cancer Commun (Lond), 2018, 38(1):50

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Phytomedicine, 2018, 39:33-41

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Int J Oncol, 2018, 52(6):2143-2154

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Purity & Quality Control

Choose Selective EGFR Inhibitors

Biological Activity

Description

Features

A potent EGFR tyrosine kinase inhibitor.

Targets

Tyr1173 (NR6W cells) ^[1]	Tyr1173 (NR6wtEGFR cells) ^[1]	Tyr992 (NR6wtEGFR cells) ^[1]	Tyr992 (NR6W cells) ^[1]
26 nM	37 nM	37 nM	57 nM

In vitro

Gefitinib effectively inhibits all tyrosine phosphorylation sites on EGFR in both the high and low-EGFR-expressing cell lines including NR6, NR6M and NR6W cell lines. The phosphorylation sites Tyr1173 and Tyr992 are less sensitive requiring higher concentrations of Gefitinib for inhibition. Gefitinib effectively blocks the phosphorylation of PLC-γ, with IC50 of 27nM, in NR6W cells. The NR6wtEGFR and NR6M cell lines has low levels of PLC-γ phosphorylation but the level in the NR6M cell line is more resistant to inhibition by Gefitinib with IC50 of 43 nM and 369 nM, respectively. Gefitinib inhibits Akt phosphorylations, with IC50 of 220 and 263nM, in the low-EGFR- and -EGFRvIII-expressing cell lines, respectively. Gefitinib in the dose range from 0.1 to 0.5μM significantly facilitates, rather than abrogates, colony formation of NR6M cells. However, at a concentration of 2 μM Gefitinib completely blocks NR6M colony formation. Gefitinib rapidly and in a dose-dependent manner inhibits EGFR and ERK phosphorylation up to 72 hours after EGF stimulation in both the high- and low-EGFR-expressing cell lines. ^[1] Gefitinib is the monolayer growth of these EGF-driven untransformed MCF10A cells with an IC50 of 20 nM. ^[2] The combination of Gefitinib (0.2 μM and 0.5 μM) with irradiation lead to a significant growth inhibition in LoVo cells, compared with radiation alone.. ^[3]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
NCI-H1975	NX3KelU4T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MnLxTWM2OD1{MT60OlEh\|ryP	NVv3XJJkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
HT	NFSzb4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MVXJR\|UxRTJzLkSzN\|Eh\|ryP	NFLJUIg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
HUTU-80	Ml;OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				Mle5TWM2OD1{MT60N\|M3KM7:TR?=	MmX5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
PA-1	Mk\QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				M1LnTWlEPTB;MkGuNlc5PyEQvF2=	NHzQfVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
HOP-62	MormS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NWDQ[3pQUUN3ME2yNU4zPzh2IN88US=>	Mli3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
GI-1	MmfkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NXXHOGtzUUN3ME2yNU4yPyEQvF2=	MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N\|kwLz6VQV7HSXI9N2F-
MC116	MmjkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				M3;vUWlEPTB;MkGuNFczOyEQvF2=	NHHpRVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
A375	MkXCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NVjjd4Q2UUN3ME2yNU4xPTZ5IN88US=>	M1fWS\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
IST-SL1	NHzlOVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NH7w[ZVKSzVyPUKwMlc5PzlizszN	MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N\|kwLz6VQV7HSXI9N2F-
TE-5	MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				M4TReWlEPTB;MkCuO\|Q5OiEQvF2=	NHrQd2M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
SiHa	MmXXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NWO5[GhXUUN3ME2yNE4{PzF{IN88US=>	MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N\|kwLz6VQV7HSXI9N2F-
LB2518-MEL	MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NFHZbnVKSzVyPUKwMlM4OzlizszN	M2nBNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
BB49-HNC	MmD5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NUfTVVFvUUN3ME2xPU46OiEQvF2=	M3jMN\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
HGC-27	NWTEZ\|lLT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MkjyTWM2OD1{MD6xN\|k1KM7:TR?=	MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N\|kwLz6VQV7HSXI9N2F-
Becker	NWe4[GRIT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				M{HweWlEPTB;MUmuPFU1PyEQvF2=	Mmr4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
TYK-nu	NXvZPXJMT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NIr5UWdKSzVyPUG5Mlg{PzhizszN	NHWwSnM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
NCI-H650	MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NIHhOItKSzVyPUG5Mlc2ODhizszN	M{XpflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
WM-115	NWDFempHT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NGrIW5NKSzVyPUG5MlY4PzRizszN	NGjvTpU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
HuH-7	Mli1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MlPNTWM2OD1zOT63OFIyKM7:TR?=	NUWwWVQyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
NCI-N87	NUfJS\|N[T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NInRPFRKSzVyPUG5MlU6QTJizszN	M{L1WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
NCI-H1048	MkP5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MVPJR\|UxRTF7LkKzNlYh\|ryP	NU\WdXpYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
NCI-H446	MnL5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NWnsN2t7UUN3ME2xPU4{PTh7IN88US=>	MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N\|kwLz6VQV7HSXI9N2F-
NCI-H1437	Mnj4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NEHabotKSzVyPUG5MlA1PjdizszN	MkT0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
D-263MG	MkHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MmTDTWM2OD1zOT6wNVczKM7:TR?=	MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N\|kwLz6VQV7HSXI9N2F-
MFH-ino	NFHmbWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MWDJR\|UxRTF6Lkm2Olkh\|ryP	M2LUW\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
U-266	Mk\iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NF3RXXBKSzVyPUG4Mlg3PDlizszN	NGH4d\|A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
OVCAR-8	M2\0Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MYTJR\|UxRTF6LkmyO\|Yh\|ryP	Mm\aQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
KNS-42	Mmf6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MWfJR\|UxRTF6LkiwNVUh\|ryP	Mme1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
U251	MoLES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				Ml;YTWM2OD1zOD63N\|Q4KM7:TR?=	NXLGXWNPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
MFE-280	MlfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NXfhNY1UUUN3ME2xPE44Ojl\|IN88US=>	Mkj0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
NCI-H1563	NE\uNplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NY\3OXM{UUN3ME2xPE44OTJ2IN88US=>	NGH2S\|I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
MDA-MB-361	NHjCZYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				Moi0TWM2OD1zOD61OVg5KM7:TR?=	MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N\|kwLz6VQV7HSXI9N2F-
HLE	M2OwUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				M2PJOWlEPTB;MUiuN\|E1QCEQvF2=	MkfRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
SW982	MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NEPKVHZKSzVyPUG4MlQxPzVizszN	NYTQfG1JRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
KM-H2	NH3JN\|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MVHJR\|UxRTF5Lkm0NVEh\|ryP	NH\xOHc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
D-502MG	M{TUWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NGrhdmFKSzVyPUG3Mlk5ODhizszN	NHrtZ5Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
ES8	M13PT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MoixTWM2OD1zNz64OVk{KM7:TR?=	NVTifXRSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
SF268	NFjoXVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				M3XEW2lEPTB;MUeuOlk3QSEQvF2=	MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N\|kwLz6VQV7HSXI9N2F-
Calu-6	MkTIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MnfsTWM2OD1zNz62O\|gzKM7:TR?=	M17CNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
SW1783	MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MWfJR\|UxRTF5Lk[0NVUh\|ryP	MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N\|kwLz6VQV7HSXI9N2F-
NCI-H747	NFnIdZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MV\JR\|UxRTF5LkWyPVch\|ryP	MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N\|kwLz6VQV7HSXI9N2F-
NCI-H1573	NGL6UIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				M3rldmlEPTB;MUeuNlgzPiEQvF2=	NVj4Vo9LRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTN7Lze+V2FPT0WUPD;hQi=>
NCI-H1581	M{W0WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MXnJR\|UxRTF5LkS0NVEh\|ryP	NFrSOmg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6OzlxJ{7TRW5ITVJ:L3G+
RKO	M3v4XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NUfXUWlSUUN3ME2xO{4xPzR6IN88US=>	MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N\|kwLz6VQV7HSXI9N2F-
MZ2-MEL	M2nud2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NUW2OHZYUUN3ME2xO{4yOzNizszN	MoDxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
GI-ME-N	MoPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MWjJR\|UxRTF4LkmwN\|Ih\|ryP	MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5N\|kwLz6VQV7HSXI9N2F-
LB373-MEL-D	NUH0[odKT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MVnJR\|UxRTF4LkeyN\|Ih\|ryP	M3\lPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
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H1975	MkC3T4lv[XOnIFHzd4F6	MYewMlUh\|ryP	NE\kZY4zPCCq	MmHiSG1UVw>?	MonG[I9meyCwb4SgbY5pcWKrdDDFS2ZTKEx6NUjSM3Q4QTCPIH31eIFvfC2vZXTpZZRm\CCDa4SgdIhwe3Cqb4L5cIF1cW:w	MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN\|OUO0Nkc,OjJ\|M{mzOFI9N2F-
H1975	NV;adoQ1U2mwYYPlJGF{e2G7	MWqwMlUh\|ryP	MlKyNlQhcA>?	NUHhfldYTE2VTx?=	MlTB[I9meyCwb4SgbY5pcWKrdDDFS2ZTKEx6NUjSM3Q4QTCPIH31eIFvfC2vZXTpZZRm\CCHcnugdIhwe3Cqb4L5cIF1cW:w	NGG3[4c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzPVM1Oid-MkKzN\|k{PDJ:L3G+
H1975	NUnSTJA5U2mwYYPlJGF{e2G7	Mm[5NE4yOjVizszN	Ml;kNlQhcA>?	MoTtSG1UVw>?	M{\3VYRw\XNibn;0JIlvcGmkaYSgSWdHWiCOOEW4Vk9VPzlyTTDteZRidnRiWUGwOlgh[XW2b4Doc5NxcG:{eXzheIlwdg>?	NIXOZYo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOzPVM1Oid-MkKzN\|k{PDJ:L3G+
H1975	Mn\MT4lv[XOnIFHzd4F6	NHvyNXoxNjN\|IN88US=>	NXXZeIpjOiCq	MYjEUXNQ	M4HiVYRw\XNibn;0JIlvcGmkaYSgSWdHWiCOOEW4Vk9VPzlyTTDkc5VjdGVibYX0ZY51KHCqb4PwbI9zgWyjdHnvci=>	NI[ybGE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEGyOFg6QCd-MkSxNlQ5QTh:L3G+
H1975	NF72OopMcW6jc3WgRZN{[Xl?	M4jNdFAvOzNizszN	MXKyJIg>	M{\GbmROW09?	NX;4bIRk\G:nczDuc5QhcW6qaXLpeEBGT0[UIFy4OVhTN1R5OUDNJIRwfWKuZTDteZRidnRiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKEWUSzDwbI9{eGixconsZZRqd25?	M{\TdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUK0PFk5Lz5{NEGyOFg6QDxxYU6=
H1975	NF\J[ZNMcW6jc3WgRZN{[Xl?	M{D4OVAvOzNizszN	M{nzblIhcA>?	NFHrd29FVVOR	MkPR[I9meyCwb4SgbY5pcWKrdDDFS2ZTKEx6NUjSM3Q4QTCPIHTveYJt\SCvdYThcpQh[XO\|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJGFMXCCyaH;zdIhwenmuYYTpc44>	NHzRb2Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEGyOFg6QCd-MkSxNlQ5QTh:L3G+
HCC827	MYPLbY5ie2ViQYPzZZk>	M1G4blAvOTFizszN	NVj0VnVuOSCq	NVHrT4M6TE2VTx?=	Mn\wbIF{KG6xIHnydoV3\XK\|aXLs[UBqdmirYnn0bY9vKG:oIFXHSnIh[XO\|ZYPz[YQh[XNicnXjc5Zmenlib3[gSWdHWiCjdYTvdIhwe3Cqb4L5cIF1cW:w	NEnNPFE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEGyOFg6QCd-MkSxNlQ5QTh:L3G+
H1975	NXfX[HU3TnWwY4Tpc44hSXO\|YYm=	MW[xJO69VQ>?	MmHCNlQhcA>?	Ml;rSG1UVw>?	NH\LTlFld2W\|IH7veEBqdmirYnn0JGVTUyCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hUDF7N{WgZ4VtdHNiaHHyZo9zcW6pIFXHSnIhVDh3OGKvWFc6OE1?	NH3OO2w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[wO\|U6OSd-MkS2NFc2QTF:L3G+
H1975	MkHkT4lv[XOnIFHzd4F6	MYexJO69VQ>?	NXvB[lF1OjRiaB?=	MmnLSG1UVw>?	MXfkc4V{KG6xdDDpcohq[mm2IFXHSnIheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGgyQTd3IHPlcIx{KGijcnLvdolv\yCHR1\SJGw5PTiUL2S3PVBOKG23dHHueC=>	MlXZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MEe1PVEoRjJ2NkC3OVkyRC:jPh?=
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A431	M1uzWGtqdmG\|ZTDBd5NigQ>?	NGiwR2YyKM7:TR?=	NGLXZZoyKGh?	M4q3fWROW09?	M13DfIhieyCwbzDpdpJmfmW{c3nicIUhcW6qaXLpeIlwdiCxZjDFS2ZTKGG3dH;wbI9{eGixconsZZRqd25?	NH7BcVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNFU6PCd-MkS5NFA2QTR:L3G+
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HCC827	M{jvemN6fG:2b4jpZ{BCe3OjeR?=	MYewMlUh\|ryP	MmfVO\|IhcA>?	M3;IfGROW09?	Mnu4bIF{KG6xIHP5eI91d3irY3n0fS=>	NIHYVGc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m5N\|MzQCd-MkO5PVM{Ojh:L3G+
HCC827	MmH1SpVv[3Srb36gRZN{[Xl?	MWKwMlUh\|ryP	MX:yJIg>	MlK1SG1UVw>?	NWn1ZWtN\G:nczDuc5QhcW6qaXLpeEBkNU2ndDDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIIC0OE81OiCyaH;zdIhwenmuYYTpc44>	NFK1SmI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m5N\|MzQCd-MkO5PVM{Ojh:L3G+
HCC827	MWnGeY5kfGmxbjDBd5NigQ>?	MWOwMlUh\|ryP	MXWyJIg>	M4jiV2ROW09?	MVzkc4V{KG6xdDDpcohq[mm2IHOtUYV1KGG\|c3Xzd4VlKGG\|IHnubIljcXSrb36gc4YhSUuWIIDoc5NxcG:{eXzheIlwdg>?	NVX1UHFvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5PVM{OjhpPkKzPVk{OzJ6PD;hQi=>
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HepG2	M2rmPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MX2yOEBp	MW\EUXNQ	NH35S\|ZKSzVyPU[uOFIh\|ryP	NW\tZWJPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3N\|EzQDFpPkK0O\|MyOjhzPD;hQi=>
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BEAS2B	MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NX7YUHhXPTBizszN	M1zJTVczKGh?	M3LMfGROW09?	MUXJR\|UxRTF\|Lkm0JO69VQ>?	MlnzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4MEe1PVEoRjJ2NkC3OVkyRC:jPh?=
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RO82-W-1	M3Szdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NVXsfnZUUUN3ME20N{43OTV\|IN88US=>	MmfCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh3N{[2N\|MoRjJ6NUe2OlM{RC:jPh?=
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LCLC-103H	NUDwcHo1T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				M3qx[WlEPTB;NEeuOFQxPCEQvF2=	M{C4WlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=
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NCI-H1703	NVm1N3QxT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				M3r0TmlEPTB;NEiuN\|M2OiEQvF2=	MnTjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVM6Nyd-U1HOS2VTRC:jPh?=
HCC1395	NH65U2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NUXOV4NVUUN3ME20PE44PDN{IN88US=>	M{\2UlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk{QS9pPmPBUmdGWjxxYU6=

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	phospho-EGFR / phospho-ERK / phospho-SRC / phospho-AKT; PubMed: 22586683 Cancer Discov Effect of overexpressing CRKL on phosphorylation levels of EGFR, ERK, AKT and SRC in response to gefitinib. HCC827 cells expressing a control vector or CRKL were exposed to gefitinib at indicated concentrations for 6 h and cell lysates were collected for immunoblotting with indicated specific antibodies. Cyclin D1/ p16 / p27 / pRb; PubMed: 18559346 J Biol Chem levels of phosphorylated and total EGFR, IGF-1R, Akt, ERK1/2, and Rb and levels of cyclin D1, p27, p16, and actin following 6- or 16-h treatment of A431 cells with combinations of 1 or 3 μm gefitinib and 3 μm NVP-ADW742. Data are representative of two independent experiments. uc-caspase-9 / c-caspase-9 / uc-caspase-3 / c-caspase-3 / uc-PARP / PARP; PubMed: 23102728 Mol Oncol Apoptosis resulting from combined treatment with gefitinib and an MEK inhibitor. (A) apoptosis relating protein induced by gefitinib and/or AZD6244 in PC‐9/wt and PC‐9/gef B4 cells. (B) Apoptosis relating protein induced by gefitinib and/or CI‐1040 in PC‐9/wt and PC‐9/gef B4 cells. (C) apoptosis relating protein induced by gefitinib and/or AZD6244 in PC‐9/gefE3 and PC‐9/gefE7 cells. (D) apoptosis relating protein induced by gefitinib and/or CI‐1040 in PC‐9/gefE3 and PC‐9/gefE7 cells. PPAR-γ; PubMed: 23409107 PLoS One Fold increase relative to control was determined after normalization with β-actin as external loading control.	22586683 18559346 23102728 23409107
Immunofluorescence	EGFR / LC3; PubMed: 31196210 J Exp Clin Cancer Res H157 and H1299 cells were treated with gefitinib, or curcumin alone, or gefitinib plus curcumin at indicated concentration for 48 h and then were fixed with methanol, immunostained with anti-EGFR (green), anti-LC3 (red), and DAPI (blue), and analyzed by confocal microscopy to determine the intracellular locations of EGFR and LC3. PPAR-γ; PubMed: 23409107 PLoS One Upregulation and nuclear accumulation of PPARγ following treatment with gefitinib (24 hs). p-EGFR / β-catenin; PubMed: 23461856 FEBS J In untreated CNE2 cells, β-catenin was located in cytoplasmic membranes and cytoplasm. Treatment with EGF (50 ng/mL) resulted in increased β-catenin nuclear staining, which was reversed by either gefitinib (1 μM) or LY294002 (15 μM).	31196210 23409107 23461856
Growth inhibition assay	GI50; PubMed: 23409107 PLoS One Dose-response of bladder cancer cell lines to EGFR inhibitor (gefitinib). The GI50 value was defined as the mean concentration of drug that generates 50% of growth inhibition as compared to controls.	23409107

In vivo

Gefitinib (100 mg/kg) improves the anti-tumor effect of radiotherapy in LoVo tumor xenografts. ^[3] Gefitinib treatment of nude mice bearing established human GEO colon cancer xenografts reveals a reversible dose-dependent inhibition of tumor growth because GEO tumors resumes the growth rate of controls at the end of the treatment. ^[4]

Protocol

Cell Research:^[1]

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Cell lines: NR6, NR6M and NR6W cells
Concentrations: 0-2 μM
Incubation Time: 72 hours
Method: Exponentially growing cells including NR6, NR6M, NR6M and NR6W cells are seeded in sextuple in 96-well plates at a concentration of 2000 cells/well, allowed to adhere and subsequently washed in PBS and incubated overnight in medium containing 0.5% FCS. Cells are then treated with varying concentrations (0-2 μM) of Gefitinib or the solute control DMSO and EGF. The optimal EGF concentration for inducing proliferation of NR6wtEGFR and NR6W cells has previously been determined and hence NR6wtEGFR and NR6W cells are supplemented with 10 nM and 0.1 nM EGF, respectively. EGF is not added to NR6 and NR6M cells. After 72 hours the amount of cells are measured by performing a MTT proliferation assay.
(Only for Reference)

Animal Research:^[3]

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Animal Models: Female nude mice (cba nu/nu) aged 8–10 weeks are intra-dermal injected with LoVo cells.
Dosages: 100 mg/kg
Administration: Once daily by oral administration (0.1 mL/10 g body weight) for 14 days
(Only for Reference)

References

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Solubility (25°C)

In vitro	DMSO	89 mg/mL (199.14 mM)
	Ethanol	4 mg/mL (8.95 mM)
	Water	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 1% CMC Na For best results, use promptly after mixing.	30mg/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 Gefitinib (ZD1839) SDF

Molecular Weight	446.90
Formula	C₂₂H₂₄ClFN₄O₃
CAS No.	184475-35-2
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	Iressa
Smiles	COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4

In vivo Formulation Calculator (Clear solution)

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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 2020-01-06)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03292133	Recruiting	Drug: EGF816\|Drug: Gefitinib	Lung Cancer	Massachusetts General Hospital\|Novartis	October 31 2017	Phase 2
NCT03122717	Active not recruiting	Drug: Gefitinib\|Drug: Osimertinib	Non-Small Cell Lung Cancer	Dana-Farber Cancer Institute\|AstraZeneca	May 9 2017	Phase 1\|Phase 2
NCT02932345	Completed	--	EGFR Mutation Positive Advanced Non-small-cell Lung Cancer	AstraZeneca	October 31 2016	--
NCT02824458	Recruiting	Drug: Apatinib\|Drug: Gefitinib\|Drug: Placebo	EGFR Tyrosine Kinase Inhibitors Plus VEGFR Inhibitors	Sun Yat-sen University	June 2016	Phase 3
NCT02804100	Unknown status	--	Carcinoma Non-Small-Cell Lung\|Bronchial Neoplasms\|Carcinoma Bronchogenic\|Lung Diseases\|Lung Neoplasms	Wenzhou Medical University	May 2016	--

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:
I try to dissolve Gefitinib (ZD1839) in 0.5% methylcellulose+0.2% Tween 80 for in vivo experiments. However, when I prepare the mixture, it forms precipitates. Exists another way to dissolve completely the compound?
Answer:
S1025 can be dissovled in both 5% DMSO+corn oil and 5% DMSO+30% PEG 300+5% Tween 80+ddH2O at 2.5 mg/ml clearly. It dissolves in DMSO not readily, please sonicate and warm it in water bath at about 45 degree, and dissolve it clearly first. Then add other solvent.

EGFR Signaling Pathway Map

EGFR Inhibitors with Unique Features

Pan EGFR Inhibitor

AZD8931 (Sapitinib) : Pan-ErbB inhibitor, EGFR/ErbB2/ErbB3, IC50=4 nM/3 nM/4 nM.
Most Potent EGFR Inhibitor

Afatinib (BIBW2992) : EGFR(wt), IC50=0.5 nM; EGFR(L858R), IC50=0.4 nM; EGFR(L858R/T790M), IC50=10 nM; HER2, IC50=14 nM.
FDA-approved EGFR Inhibitor

Lapatinib : Approved by FDA for breast cancer.
Newest EGFR Inhibitor

CO-1686 (AVL-301) ^New : Irreversible, mutant-selective EGFR inhibitor with K_i of 21.5 nM and 303.3 nM for EGFRL858R/T790M and EGFRWT, respectively.

Related EGFR Products

Erlotinib ^New

Erlotinib (CP358774, NSC 718781) is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. Erlotinib induces autophagy.
Afatinib (BIBW2992) Dimaleate ^New

Afatinib (BIBW2992) Dimaleate irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant. Afatinib (BIBW2992) Dimaleate induces autophagy.
Poziotinib (HM781-36B) ^New

Poziotinib (HM781-36B, NOV120101) is an irreversible pan-HER inhibitor with IC50 of 3.2 nM, 5.3 nM and 23.5 nM for HER1, HER2, and HER4, respectively. Poziotinib also induces apoptosis and G1 cell cycle arrest. Phase 2.
Erlotinib HCl (OSI-744)

Erlotinib HCl (OSI-744, CP358774, NSC 718781) is an EGFR inhibitor with IC50 of 2 nM in cell-free assays, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.
Afatinib (BIBW2992)

Afatinib (BIBW2992) inhibits EGFR/ErbB irreversibly in vitro with IC50 of 0.5, 0.4, 10, 14, 1 nM for EGFR^wt, EGFR^L858R, EGFR^L858R/T790M ErbB2 (HER2) and ErbB4 (HER4), respectively. Afatinib induces autophagy.
Osimertinib (AZD9291)

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.
Lapatinib

Lapatinib (GSK572016), used in the form of Lapatinib Ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib induces ferroptosis and autophagic cell death.
AG-490 (Tyrphostin B42)

AG-490 (Tyrphostin B42, Zinc02557947) is an inhibitor of EGFR with IC50 of 0.1 μM in cell-free assays, 135-fold more selective for EGFR versus ErbB2, also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src.
Rociletinib (CO-1686)

Rociletinib (CO-1686, AVL-301) is an irreversible, mutant-selective EGFR inhibitor with K_i of 21.5 nM and 303.3 nM for EGFR^L858R/T790M and EGFR^WT in cell-free assays, respectively. Phase 2.
AG-1478 (Tyrphostin AG-1478)

AG-1478 (Tyrphostin AG-1478, NSC 693255) is a selective EGFR inhibitor with IC50 of 3 nM in cell-free assays, almost no activity on HER2-Neu, PDGFR, Trk, Bcr-Abl and InsR. AG-1478 (Tyrphostin AG-1478) inhibits encephalomyocarditis virus (EMCV) and hepatitis c virus (HCV) by targeting phosphatidylinositol 4-kinase IIIα (PI4KA).

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Gefitinib (ZD1839)