ABT-737

Name: ABT-737
Brand: Selleck Chemicals
SKU: S1002
Rating: 5 (212 reviews)

For research use only. Not for use in humans.

Catalog No.S1002

212 publications

Molecular Weight(MW): 813.43

ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. Phase 2.

Selleck's ABT-737 has been cited by 212 publications

Cell, 2018, 175(2):429-441

PubMed: 30245008 ( click the link to review the publication )

Cancer Cell, 2018, 33(3):435-449

PubMed: 29533784 ( click the link to review the publication )

Nature, 2017, 551(7679):247-250

PubMed: 29088702 ( click the link to review the publication )

Nat Methods, 2017, 14(9):891-896

PubMed: 28737741 ( click the link to review the publication )

Nature, 2016, 529(7586):413-417

PubMed: 26735014 ( click the link to review the publication )

Nat Med, 2013, 19(11):1478-88

PubMed: 24141421 ( click the link to review the publication )

Nat Biotechnol, 2011, 29(6):542-6

PubMed: 21623355 ( click the link to review the publication )

Am J Respir Crit Care Med, 2019, 200(1):84-97

PubMed: 30649895 ( click the link to review the publication )

Mol Cell, 2019, 74(1):19-31

PubMed: 30878284 ( click the link to review the publication )

Nat Commun, 2019, 10(1):5770

PubMed: 31852899 ( click the link to review the publication )

EMBO J, 2019, 38(11)

PubMed: 30979778 ( click the link to review the publication )

Dev Cell, 2019, 51(2):277-291

PubMed: 31564612 ( click the link to review the publication )

Cancer Res, 2019, 79(9):2339-2351

PubMed: 30862722 ( click the link to review the publication )

Cell Rep, 2019, 27(12):3657-3671

PubMed: 31216482 ( click the link to review the publication )

Cell Rep, 2019, 27(3):820-834

PubMed: 30995479 ( click the link to review the publication )

Br J Pharmacol, 2019, 176(3):436-450

PubMed: 30427531 ( click the link to review the publication )

Cancers (Basel), 2019, 11(9)

PubMed: 31540244 ( click the link to review the publication )

Cancers (Basel), 2019, 11(12)

PubMed: 31810230 ( click the link to review the publication )

J Cancer, 2019, 10(6):1466-1478

PubMed: 31031856 ( click the link to review the publication )

Thromb Haemost, 2019, 19(10):1665-1674

PubMed: 31493778 ( click the link to review the publication )

Eur J Immunol, 2019, 10.1002/eji.201948254

PubMed: 31411729 ( click the link to review the publication )

Phytomedicine, 2019, 64:153068

PubMed: 31419729 ( click the link to review the publication )

Phytomedicine, 2019, 52:147-156

PubMed: 30599894 ( click the link to review the publication )

Chem Biol Interact, 2019, 309:108723

PubMed: 31228469 ( click the link to review the publication )
J Bone Oncol, 2019, 19:100268

PubMed: 31832331 ( click the link to review the publication )

J Bone Oncol, 2019, 15:100222

PubMed: 30766792 ( click the link to review the publication )

Onco Targets Ther, 2019, 12:897-906

PubMed: 30774376 ( click the link to review the publication )

Platelets, 2019, 30(1):75-80

PubMed: 29125379 ( click the link to review the publication )

Immunity, 2018, 48(4):675-687

PubMed: 29653696 ( click the link to review the publication )

Nat Commun, 2018, 9(1):5435

PubMed: 30575733 ( click the link to review the publication )

Clin Cancer Res, 2018, 24(21):5458-5470

PubMed: 30021909 ( click the link to review the publication )

Oncogene, 2018, 37(39):5325-5339

PubMed: 29858601 ( click the link to review the publication )

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

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

Cell Death Dis, 2018, 9(10):944

PubMed: 30237504 ( click the link to review the publication )

Cell Death Dis, 2018, 9(2):123

PubMed: 29374144 ( click the link to review the publication )

Cell Death Dis, 2018, 9(10):994

PubMed: 30250198 ( click the link to review the publication )

Cell Death Dis, 2018, 9(2):199

PubMed: 29415991 ( click the link to review the publication )

Cell Death Dis, 2018, 92(10)

PubMed: 23640461 ( click the link to review the publication )

Biochim Biophys Acta Mol Cell Res, 2018, 1865(3):522-531

PubMed: 29278689 ( click the link to review the publication )

Mol Cancer Res, 2018, 16(6):935-946

PubMed: 29545477 ( click the link to review the publication )

Antioxidants (Basel), 2018, 10.3390/antiox7110150

PubMed: 30373097 ( click the link to review the publication )

Cancer Biol Ther, 2018, 19(6):465-474

PubMed: 29394130 ( click the link to review the publication )

Phytother Res, 2018, 32(6):1126-1134

PubMed: 29464855 ( click the link to review the publication )

Thromb Res, 2018, 171:22-30

PubMed: 30240944 ( click the link to review the publication )

Oncotarget, 2018, 9(24):16701-16717

PubMed: 29682179 ( click the link to review the publication )

Oncotarget, 2018, 9(39):25630-25646

PubMed: 29876013 ( click the link to review the publication )

Oncotarget, 2018, 9(42):26834-26851

PubMed: 29928488 ( click the link to review the publication )

Nat Cell Biol, 2017, 19(10):1226-1236

PubMed: 28945232 ( click the link to review the publication )
Nat Cell Biol, 2017, 19(9):1116-1129

PubMed: 28846096 ( click the link to review the publication )

J Clin Invest, 2017, 127(1):153-168

PubMed: 27893461 ( click the link to review the publication )

J Clin Invest, 2017, 127(2):635-650

PubMed: 28094768 ( click the link to review the publication )

Nat Commun, 2017, 8:16078

PubMed: 28714472 ( click the link to review the publication )

Genes Dev, 2017, 31(17):1754-1769

PubMed: 28982759 ( click the link to review the publication )

Elife, 2017, 6

PubMed: 28692422 ( click the link to review the publication )

Elife, 2017, 6

PubMed: 29148970 ( click the link to review the publication )

Oncogene, 2017, 36(15):2066-2073

PubMed: 27694901 ( click the link to review the publication )

Cancer Lett, 2017, 411:19-26

PubMed: 28987383 ( click the link to review the publication )

Arch Toxicol, 2017, 91(5):2191-2208

PubMed: 27807597 ( click the link to review the publication )

Biochem Pharmacol, 2017, 140:41-52

PubMed: 28595877 ( click the link to review the publication )

Analyst, 2017, 142(23):4399-4404

PubMed: 29116264 ( click the link to review the publication )

Toxicol In Vitro, 2017, 42:38-46

PubMed: 28366708 ( click the link to review the publication )

Mol Cell Biochem, 2017, 429(1-2):91-102

PubMed: 28120212 ( click the link to review the publication )

Arch Oral Biol, 2017, 73:1-6

PubMed: 27632413 ( click the link to review the publication )

Oncol Lett, 2017, 14(1):903-908

PubMed: 28693250 ( click the link to review the publication )

Asia Pac J Clin Oncol, 2017, 13(2):e144-e152

PubMed: 26552712 ( click the link to review the publication )

Oncotarget, 2017, 8(29):46801-46817

PubMed: 27086916 ( click the link to review the publication )

Oncotarget, 2017, 8(63):107206-107222

PubMed: 29291023 ( click the link to review the publication )

Thromb Haemost, 2017, 117(2):311-324

PubMed: 27929199 ( click the link to review the publication )

J Clin Invest, 2016, 126(1):181-94

PubMed: 26619119 ( click the link to review the publication )

Nat Commun, 2016, 7:11190

PubMed: 27048913 ( click the link to review the publication )

Autophagy, 2016, 12(7):1083-93

PubMed: 27172402 ( click the link to review the publication )

Clin Cancer Res, 2016, 22(5):1138-49

PubMed: 26467384 ( click the link to review the publication )
Br J Pharmacol, 2016, 173(3):471-83

PubMed: 26493374 ( click the link to review the publication )

Br J Cancer, 2016, 114(11):1219-26

PubMed: 27140314 ( click the link to review the publication )

Oncogenesis, 2016, 10.1038/oncsis.2016.33

PubMed: 27159675 ( click the link to review the publication )

J Virol, 2016, 90(5):2356-71

PubMed: 26676786 ( click the link to review the publication )

Biochim Biophys Acta, 2016, 1863(4):562-71

PubMed: 26704388 ( click the link to review the publication )

Lab Invest, 2016, 96(10):1128-37

PubMed: 27617402 ( click the link to review the publication )

Am J Cancer Res, 2016, 6(6):1345-57

PubMed: 27429848 ( click the link to review the publication )

Cancer Cell Int, 2016, 16:27

PubMed: 27042160 ( click the link to review the publication )

Biochem Biophys Res Commun, 2016, 477(4):607-13

PubMed: 27343560 ( click the link to review the publication )

Biochem Biophys Res Commun, 2016, 478(1):143-148

PubMed: 27449608 ( click the link to review the publication )

Anticancer Res, 2016, 36(4):1673-82

PubMed: 27069145 ( click the link to review the publication )

Exp Ther Med, 2016, 11(2):669-673

PubMed: 26893664 ( click the link to review the publication )

Sci Rep, 2016, 6:21264

PubMed: 26887909 ( click the link to review the publication )

Oncotarget, 2016, 7(3):3520-32

PubMed: 26657288 ( click the link to review the publication )

Tumour Biol, 2016, 37(8):10839-49

PubMed: 26880588 ( click the link to review the publication )

Oncotarget, 2016, 7(51):85492-85501

PubMed: 27863431 ( click the link to review the publication )

Oncotarget, 2016, 7(51):84594-84607

PubMed: 27829238 ( click the link to review the publication )

Oncotarget, 2016, 7(50):83208-83222

PubMed: 27825124 ( click the link to review the publication )

Oncotarget, 2016, 7(6):6626-38

PubMed: 26675547 ( click the link to review the publication )

Oncotarget, 2016, 7(47):77815-77824

PubMed: 27780925 ( click the link to review the publication )

Nat Commun, 2015, 6:6891

PubMed: 25922916 ( click the link to review the publication )

Autophagy, 2015, 11(3):452-9

PubMed: 25715028 ( click the link to review the publication )

Clin Cancer Res, 2015, 21(17):3995-4003

PubMed: 26015514 ( click the link to review the publication )

Cell Death Differ, 2015, 10.1038/cdd.2015.8

PubMed: 25698446 ( click the link to review the publication )
Mol Oncol, 2015, 9(2):409-21

PubMed: 25308513 ( click the link to review the publication )

Mol Oncol, 2015, 9(2):409-21

PubMed: ( click the link to review the publication )

J Biol Chem, 2015, 290(19):12290-9

PubMed: 25829495 ( click the link to review the publication )

Cancer Cell Int, 2015, 15:34

PubMed: 25852302 ( click the link to review the publication )

Neurogastroenterol Motil, 2015, 10.1111/nmo.12521

PubMed: 25690069 ( click the link to review the publication )

Int J Oncol, 2015, 46(2):667-76

PubMed: 25434832 ( click the link to review the publication )

Eur J Pharm Sci, 2015, 70:64-71

PubMed: ( click the link to review the publication )

Eur J Pharm Sci, 2015, 70:64-71

PubMed: 25596561 ( click the link to review the publication )

Hepatol Res, 2015, 45(9):1023-1033

PubMed: 25297967 ( click the link to review the publication )

Exp Cell Res, 2015, 335(1):62-7

PubMed: 26024774 ( click the link to review the publication )

Exp Cell Res, 2015, 10.1016/j.yexcr.2015.04.016

PubMed: 25936772 ( click the link to review the publication )

BMC Cancer, 2015, 15:919

PubMed: 26585594 ( click the link to review the publication )

PLoS One, 2015, 10(11):e0143685

PubMed: 26606677 ( click the link to review the publication )

Biochem Biophys Res Commun, 2015, 464(1):286-91

PubMed: 26116776 ( click the link to review the publication )

Mutation Research/Fundamental and Molecular Mechanisms of Mutagenesis, 2015, 10.1016/j.mrfmmm.2015.04.005

PubMed: ( click the link to review the publication )

Anticancer Res, 2015, 35(3):1803-8

PubMed: 25750346 ( click the link to review the publication )

Oncotarget, 2015, 6(34):36338-53

PubMed: 26462148 ( click the link to review the publication )

Arch Pharm Chem Life Sci, 2015, 348: 1-11

PubMed: 25641608 ( click the link to review the publication )

Oncotarget, 2015, 6(1):409-26

PubMed: 25565667 ( click the link to review the publication )

Oncotarget, 2015, 6(8):5582-96

PubMed: 25714024 ( click the link to review the publication )

Oncotarget, 2015, 6(14):12405-20

PubMed: 25915159 ( click the link to review the publication )

Nat Commun, 2014, 5:5637

PubMed: 25472497 ( click the link to review the publication )

Autophagy, 2014, 10(10):1776-86

PubMed: 25126729 ( click the link to review the publication )

Clin Cancer Res, 2014, 20(21):5446-55

PubMed: 25208882 ( click the link to review the publication )
Leukemia, 2014, 28(10):1960-8

PubMed: 24577530 ( click the link to review the publication )

Chem Sci, 2014, 5, 2794–2803

PubMed: ( click the link to review the publication )

Biomaterials, 2014, 16(2):R41

PubMed: 24745479 ( click the link to review the publication )

Cell Death Differ, 2014, 21(7):1170-7

PubMed: 24682005 ( click the link to review the publication )

Cell Death Differ, 2014, 10.1038/cdd.2014.158

PubMed: 25301069 ( click the link to review the publication )

Cancer Lett, 2014, 10.1016/j.canlet.2014.09.024

PubMed: 25304383 ( click the link to review the publication )

Cancer Lett, 2014, 348(1-2):38-49

PubMed: 24650799 ( click the link to review the publication )

Biomaterials Science, 2014, 10.1039/C4BM00072B

PubMed: ( click the link to review the publication )

Cell Death Dis, 2014, 5:e1445

PubMed: 25299770 ( click the link to review the publication )

Cell Death Dis, 2014, 5:e1291

PubMed: 24922075 ( click the link to review the publication )

Cell Death Dis, 2014, 5:e1275

PubMed: 24901046 ( click the link to review the publication )

Acta Neuropathol Commun, 2014, 10.1186/2051-5960-2-57

PubMed: 24887326 ( click the link to review the publication )

Mol Cancer Ther, 2014, 10.1158/1535-7163.MCT-13-0998

PubMed: 24739394 ( click the link to review the publication )

Mol Cancer Res, 2014, 13(12):3332-42

PubMed: 25154561 ( click the link to review the publication )

Mol Cancer Res, 2014, (4):550-9

PubMed: 24469836 ( click the link to review the publication )

J Immunol, 2014, 193(10):4914-23

PubMed: 25288570 ( click the link to review the publication )

Bone, 2014, 67:166-74

PubMed: 25016096 ( click the link to review the publication )

J Biol Chem, 2014, 289(22):15495-15506

PubMed: 24739390 ( click the link to review the publication )

J Immunother, 2014, 37(1):8-15

PubMed: 24316551 ( click the link to review the publication )

Int J Mol Sci, 2014, 15(11):20500-17

PubMed: 25387078 ( click the link to review the publication )

Int J Hyperthermia, 2014, 30(7):502-12

PubMed: 25354679 ( click the link to review the publication )

Cell Cycle, 2014, 10.4161/15384101.2014.973321

PubMed: ( click the link to review the publication )

Thromb Res, 2014, 134(6):1311-5

PubMed: 25288466 ( click the link to review the publication )

Thromb Res, 2014, 133(1):73-9

PubMed: 24268298 ( click the link to review the publication )
PLoS One, 2014, 9(9):e103015

PubMed: 25181509 ( click the link to review the publication )

PLoS One, 2014, 9(1):e84388

PubMed: 24427286 ( click the link to review the publication )

PLoS One, 2014, 9(9):e106571

PubMed: 25192188 ( click the link to review the publication )

PLoS One, 2014, 9(2):e88587

PubMed: 24523919 ( click the link to review the publication )

PLoS One, 2014, 9(8):e105049

PubMed: 25126950 ( click the link to review the publication )

PLoS One, 2014, 9(3):e91782

PubMed: 24626299 ( click the link to review the publication )

PLoS One, 2014, 9(5):e96733

PubMed: 24824755 ( click the link to review the publication )

Leuk Lymphoma, 2014, 5:1-12

PubMed: 25373508 ( click the link to review the publication )

Biomed Res Int, 2014, 2014:306718

PubMed: ( click the link to review the publication )

Int J Cancer, 2013, 133(8):1813-24

PubMed: 23580240 ( click the link to review the publication )

J Neurosci, 2013, 33(46):18098-108

PubMed: 24227720 ( click the link to review the publication )

Cell Death Dis, 2013, 4:e702

PubMed: 23828565 ( click the link to review the publication )

Cell Death Dis, 2013, 4:e762

PubMed: 23928701 ( click the link to review the publication )

Br J Cancer, 2013, 108(9):1870-8

PubMed: 23558901 ( click the link to review the publication )

Cell Death Dis, 2013, 4:e690

PubMed: 23807219 ( click the link to review the publication )

Cell Death Dis, 2013, 4:e801

PubMed: 24030153 ( click the link to review the publication )

Cell Death Dis, 2013, 4:e742

PubMed: 23887633 ( click the link to review the publication )

Br J Haematol, 2013, 163(3):377-84

PubMed: 24033315 ( click the link to review the publication )

Br J Haematol, 2013, 161(2):245-54

PubMed: 23398569 ( click the link to review the publication )

Stem Cells Transl Med, 2013, 2(9):690-702

PubMed: 23934910 ( click the link to review the publication )

Cancer Sci, 2013, 104(6):732-9

PubMed: 23421409 ( click the link to review the publication )

Mol Cancer Res, 2013, 11(2):109-21

PubMed: 23233484 ( click the link to review the publication )

Cancer Gene Ther, 2013, 20(7):386-93

PubMed: 23788110 ( click the link to review the publication )

J Biol Chem, 2013, 288(10):6826-34

PubMed: 23329846 ( click the link to review the publication )
Apoptosis, 2013, 18(11):1403-15

PubMed: 23760752 ( click the link to review the publication )

Biomed Pharmacother, 2013, 67(7):583-91

PubMed: 23706691 ( click the link to review the publication )

Toxicol Appl Pharmacol, 2013, 274(2):319-27

PubMed: 24321340 ( click the link to review the publication )

Int J Biochem Cell Biol, 2013, 45(5):944-51

PubMed: 23395630 ( click the link to review the publication )

PLoS One, 2013, 8(11):e78570

PubMed: 24223823 ( click the link to review the publication )

Biochem Biophys Res Commun, 2013, 437(4):565-72

PubMed: 23850692 ( click the link to review the publication )

Leuk Lymphoma, 2013, 54(2):372-80

PubMed: 22830613 ( click the link to review the publication )

Exp Dermatol, 2013, 22(8):518-23

PubMed: 23802633 ( click the link to review the publication )

Basic Clin Pharmacol Toxicol, 2013, 113(3):145-51

PubMed: 23557083 ( click the link to review the publication )

J Ovarian Res, 2013, 6(1):72

PubMed: 24103422 ( click the link to review the publication )

Cytometry A, 2013, 83(2):227-34

PubMed: 23165976 ( click the link to review the publication )

Blood, 2012, 120(19):3978-85

PubMed: 22927247 ( click the link to review the publication )

Mol Cell, 2012, 46(5):573-83

PubMed: 22560721 ( click the link to review the publication )

J Clin Invest, 2012, 122(6):2018-31

PubMed: 22622039 ( click the link to review the publication )

EMBO J, 2012, 31(10):2322-35

PubMed: 22510886 ( click the link to review the publication )

Oncogene, 2012, 31(26):3177-89

PubMed: 22056880 ( click the link to review the publication )

Breast Cancer Res, 2012, 14(3):R96

PubMed: 22703841 ( click the link to review the publication )

Anal Chem, 2012, 84(11):4703-10

PubMed: 22533353 ( click the link to review the publication )

Br J Haematol, 2012, 159(5):565-71

PubMed: 23025479 ( click the link to review the publication )

Mol Cancer Res, 2012, 10(3):347-59

PubMed: 22241218 ( click the link to review the publication )

J Biol Chem, 2012, 287(25):21357-70

PubMed: 22553204 ( click the link to review the publication )

J Biol Chem, 2012, 287(21):17682-92

PubMed: 22433870 ( click the link to review the publication )

Mol Endocrinol, 2012, 26(9):1508-20

PubMed: 22771494 ( click the link to review the publication )

Phytother Res, 2012, 27(6):835-40

PubMed: 22899281 ( click the link to review the publication )
BMC Cancer, 2012, 12:541

PubMed: 23171055 ( click the link to review the publication )

PLoS One, 2012, 7(8):e43158

PubMed: 22912816 ( click the link to review the publication )

PLoS One, 2012, 7(12):e52333

PubMed: 23284992 ( click the link to review the publication )

J Pharmacol Sci, 2012, 119(4):330-40

PubMed: 22814102 ( click the link to review the publication )

Blood, 2011, 117(26):7145-54

PubMed: 21562047 ( click the link to review the publication )

J Clin Invest, 2011, 121(3):1053-63

PubMed: 21317538 ( click the link to review the publication )

Leukemia, 2011, 25(11):1728-38

PubMed: 21701487 ( click the link to review the publication )

Neuro Oncol, 2011, 13(12):1265-76

PubMed: 21880625 ( click the link to review the publication )

Cancer Res, 2011, 71(13):4494-505

PubMed: 21555370 ( click the link to review the publication )

Oncogene, 2011, 30(37):3918-29

PubMed: 21460857 ( click the link to review the publication )

Am J Nephrol, 2011, 34(6):549-59

PubMed: 22123611 ( click the link to review the publication )

Cancer Chemoth Pharm, 2011, 67(3):557-67

PubMed: 20473610 ( click the link to review the publication )

PLoS One, 2011, 6(6):e20423

PubMed: 21674052 ( click the link to review the publication )

PLoS One, 2011, 6(9):e24102

PubMed: 21949692 ( click the link to review the publication )

Biochem Biophys Res Commun, 2011, 408(2):344-9

PubMed: 21514278 ( click the link to review the publication )

Curr Pharmacogenomics Person Med, 2011, 9(3):184-190

PubMed: 22162984 ( click the link to review the publication )

Mol Cancer Ther, 2010, 19(20):5591-601

PubMed: 20587662 ( click the link to review the publication )

J Biol Chem, 2010, 285(26):19910-20

PubMed: 20421300 ( click the link to review the publication )

Apoptosis, 2010, 15(10):1256-69

PubMed: 20582477 ( click the link to review the publication )

Exp Hematol, 2010, 38(10):908-921

PubMed: 20540984 ( click the link to review the publication )

Purity & Quality Control

Choose Selective Bcl-2 Inhibitors

Biological Activity

Description

Features

First-generation inhibitor of anti-apoptotic Bcl-2 proteins.

Targets

Bcl-2 ^[1] (Cell-free assay)	Bcl-xL ^[1] (Cell-free assay)	Bcl-w ^[1] (Cell-free assay)	Bcl-B ^[1] (Cell-free assay)
30.3 nM(EC50)	78.7 nM(EC50)	197.8 nM(EC50)	1.82 μM(EC50)

In vitro

ABT-737 shows low activity to Bcl-B and no effects to Mcl-1 and BFL-1. ABT-737 is sensitive to HL60, KG1 and NB4 cells with IC50 of 50 nM, 80 nM and 80 nM, respectively. ABT-737 induces apoptosis in HL60 cells, which due to decreased Bcl-2/Bax heterodimerization and has no effect on cell cycle distribution. ABT-737 also induces cytochrome c release from purified mitochondria and promotes conformational changes in Bax that are associated with apoptosis. ^[1] Resistant cells (Hela and MCF-7) can be sensitized to ABT-737 by approaches that down-regulate, destabilize, or inactivate Mcl-1. ABT-737 also causes Bax/BAK-dependent cytochrome c release only when Mcl-1 has been neutralized. ^[2] ABT-737 displaces Bim from Bcl2's BH3-binding pocket, allowing Bim to activate Bax, induce mitochondrial permeabilization, and rapidly commit the primary chronic lymphocytic leukemia (CLL) cells to death. ^[3] Knockdown of Mcl-1 with siRNA sensitizes two resistant SCLC cell lines H196 and DMS114 to ABT-737 by enhancing the induction of apoptosis. Likewise, up-regulation of Noxa sensitizes H196 cells to ABT-737. ABT-737 inhibits proliferation and induces apoptosis in many SCLC cell lines including NCI-H889, NCI-H1963, NCI-H1417, NCI-H146 and etc. Bcl-2 and Noxa may contribute mechanistically to the cellular response to ABT-737 in NCI-H146 cells. ^[4] A recent study shows that ABT-737 significantly induces apoptosis in HTLV-1 infected T-cell lines as well as in fresh ATLL cells. ^[5]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
OCI-Ly1	MUnD[YxtKF[rYXLpcIl1gSCDc4PhfS=>	MnLmNlUxKG6PwrC=	NXuyVokxPzJiaB?=	NUTxbpp7TE2VTx?=	NFHpZXhk[XW\|ZXSgPVcmKGyxc4Ogc4YhfmmjYnnsbZR6KGmwIHPlcIx{KHS{YX7z[oVkfGWmIIfpeIghSkOONjDzbXJPSQ>?	NXrDVFZjOjZ4NUeyPFg>
KG1a	M2rGNGNmdGxiVnnhZoltcXS7IFHzd4F6	M37ieVAuOTBizszN	MV[yOEBp	NV3FVGdxTE2VTx?=	MonZTWM2OD15Lk[4JO69VSxiZHXjdoVie2W\|IHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz	MWiyOlU2OjdzMh?=
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HCT116	MVPD[YxtKF[rYXLpcIl1gSCDc4PhfS=>	Ml61NE0yOCEQvF2=	MnnYNlTjiImqwrC=	MleySG1UVw>?	M4H4cmlEPTB;MkCuOFnjiIoEtV2=	M3zzS\|I2OzB2M{iz
HaCaT	MV3D[YxtKF[rYXLpcIl1gSCDc4PhfS=>	NHjtVHYxNjFxMT:xNEDPxE1?	NIezS5MzPCCq	Mo\USG1UVw>?	M3;UNoRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?=	MXSyOVIyODd7NR?=
A5-RT3	NFmwSVFE\WyuIG\pZYJqdGm2eTDBd5NigQ>?	NULZfpFUOC5zL{GvNVAh\|ryP	NHLYd3YzPCCq	MYrEUXNQ	M{\Jd4Rm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?=	MlzzNlUzOTB5OUW=
HaCaT	MXLGeY5kfGmxbjDBd5NigQ>?	MXixNQKBkc7:TR?=	NEDTbpMzPC92ODDo	NEjLV3VFVVOR	M2r6folv\HWlZYOgUW1RKGGwZDDEUmEh\nKjZ33lcpRifGmxbh?=	NEfMXmczPTJzMEe5OS=>
A5-RT3	M2HKRmZ2dmO2aX;uJGF{e2G7	NVj2fJNKOTEkgJpOwG0>	M1fjblI1NzR6IHi=	NFLYWYVFVVOR	NIHNfFJqdmS3Y3XzJG1OWCCjbnSgSG5CKG[{YXft[Y51[XSrb36=	NHrSd2UzPTJzMEe5OS=>
A5-RT3	NUnzZoROTnWwY4Tpc44hSXO\|YYm=	NXzwTZRkPSEQvF2=	MW[2JIg>	NFT3bIlFVVOR	M4jhZYlv\HWlZYOgeIhmKHKnbHXhd4Uhd2ZibXn0c4Npd26mcnnhcEBxem:2ZXnud{BidmRicnXkeYNmeyClbH;uc4dmdmmlIIP1dpZqfmGuIHnuJIEh[2G\|cHHz[U1qdmSncHXu[IVvfCCvYX7u[ZI>	MXyyOVIyODd7NR?=
U266	M{m5[WZ2dmO2aX;uJGF{e2G7	MlzwOVAxNzd3MDDuUS=>	M4XublI1NzR6IHi=	NFfBbIhFVVOR	NVfDdINj\G:5boLl[5Vt[XSnczDCbY0tKHC{aX7jbZBidGy7IITo[UBGVCCrc3;mc5Ju	M3n0SVI2OjB6OEi4
RPMI8226	NUTxVpB{TnWwY4Tpc44hSXO\|YYm=	NWTrPZFPPTByL{e1NEBvVQ>?	NI\H[lYzPC92ODDo	NGnpd5JFVVOR	MkG3[I94dnKnZ4XsZZRmeyCEaX2sJJBzcW6laYDhcIx6KHSqZTDFUEBqe2:ob4Lt	NWDsVZdNOjV{MEi4PFg>
MM.1S	MmW5SpVv[3Srb36gRZN{[Xl?	M4DzflUxOC95NUCgcm0>	MUSyOE81QCCq	NFHyOZBFVVOR	MmTT[I94dnKnZ4XsZZRmeyCEaX2sJJBzcW6laYDhcIx6KHSqZTDFUEBqe2:ob4Lt	MUiyOVIxQDh6OB?=
Clone A	MnvwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NF31VZQxNjMkgKO2NEDPxE1?	M3PYb\|czKGh?	MnnaSG1UVw>?	M33nW2lEPTB;Nz61JO69VQ>?	MYmyOVIxQDh6Mh?=
CX-1	MnO4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NU\0[nJiOC5{4pETOlAh\|ryP	NGixR2c4OiCq	M2TYXGROW09?	MnjRTWM2OD1zLkig{txO	NYWxSHlWOjV{MEi4PFI>
LS174T	MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MlnkNE4z6oDVNkCg{txO	NHjJZW84OiCq	NV3jb\|BPTE2VTx?=	MUPJR\|UxRTF6LkOg{txO	MUKyOVIxQDh6Mh?=
HT29	NWPIcGJ1SXCxcITvd4l{KEG\|c3H5	MlT6NU82NzFyIN88US=>	NEnMVJc1QCCq		M1P0O4NifXOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy	M4[xTFI2OTl{MUi4
SW480	MnrwRZBweHSxc3nzJGF{e2G7	MnHjNU82NzFyIN88US=>	MV60PEBp		M4nvSINifXOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy	MWqyOVE6OjF6OB?=
Colo205	M1LrbGFxd3C2b4Ppd{BCe3OjeR?=	NG[2b4UyNzVxMUCg{txO	NXjB[VlEPDhiaB?=		Ml3qZ4F2e2W\|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK=	NYnWWIlIOjVzOUKxPFg>
Caco2	MVTBdI9xfG:\|aYOgRZN{[Xl?	MoG5NU82NzFyIN88US=>	MV[0PEBp		M1WxUoNifXOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy	MmLmNlUyQTJzOEi=
PCI-13	MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NIG3eY44OiCq	NWPCeFJrTE2VTx?=	NIfBc4NIUTVyPUG1JOKyKDFwODFOwG0>	NHHqTVMzPTF\|OUO4Oy=>
PCI-15B	M4X5Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NU\LeW9HPzJiaB?=	M4jKV2ROW09?	NV7zVXFLT0l3ME2xNUDDuSB2LkWg{txO	NGi0c4wzPTF\|OUO4Oy=>
UM-SCC22B	NXrMNVZpT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NVvwWld4PzJiaB?=	MWjEUXNQ	NFPsbI1IUTVyPUG5JOKyKDJwOTFOwG0>	MVKyOVE{QTN6Nx?=
UM-SCC47	MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MlzlO\|IhcA>?	MYPEUXNQ	MlPrS2k2OD1zOTFCtUAyOi5\|IN88US=>	NHfxcpUzPTF\|OUO4Oy=>
93-VU-147T	NIDrbIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NIe2bIM4OiCq	NES0U5NFVVOR	MkflS2k2OD12LkOgxtEhOy53IN88US=>	MnfvNlUyOzl\|OEe=
UD-SCC2	MkK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MY[3NkBp	M3TpWmROW09?	NYPrXJVYT0l3ME2yPEDDuSB{Lkmg{txO	NYLuXpN[OjVzM{mzPFc>
UPCI:SCC90	NHu1WINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NI\3PFM4OiCq	NWeyUIdzTE2VTx?=	NIfRdY9IUTVyPU[uOkDDuSBzLkWg{txO	M2fifFI2OTN7M{i3
RPMI-8226	MXzD[YxtKF[rYXLpcIl1gSCDc4PhfS=>	MYmxNlUwOjVyL{WwNEBvVQ>?	NHzYdYw1QGkEoB?=	MVXEUXNQ	NFTpSFRl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK=	MXmyOVAxQDJyMh?=
OPM-2	MkfTR4VtdCCYaXHibYxqfHliQYPzZZk>	MW[xNlUwOjVyL{WwNEBvVQ>?	MYK0PIjDqA>?	MnvtSG1UVw>?	Mkm2[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:\|ZT3k[ZBmdmSnboSgcYFvdmW{	NIDYbW4zPTByOEKwNi=>
RPMI-8226	MlP2RZBweHSxc3nzJGF{e2G7	M164VFEzPS9{NUCvOVAxKG6P	NGnqOI81QGkEoB?=	NGHGSoJFVVOR	M{[2O4lv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?	MnvVNlUxODh{MEK=
OPM-2	NGW4fHhCeG:ydH;zbZMhSXO\|YYm=	NUC3cXUzOTJ3L{K1NE82ODBibl2=	MUm0PIjDqA>?	NIrGWYNFVVOR	M3XN[olv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?	M{nqW\|I2ODB6MkCy
COG-LL-319	MVzGeY5kfGmxbjDBd5NigQ>?	NWjwV\|JDOTByIH7N	NXHX[oVsOS9\|L{[gbC=>	NUDab\|AyTE2VTx?=	NWj4VlBscW6mdXPld{Bk[XOyYYPlMYRmeGWwZHXueEBO[2xvMTDjcIVifmGpZR?=	M2H1V\|I1QTVzNEey
RS4;11	NVvnVFVOTnWwY4Tpc44hSXO\|YYm=	NYOyXmplOTByIH7N	Mnv2NU8{NzZiaB?=	NIHMN2RFVVOR	MorGbY5lfWOnczDjZZNx[XOnLXTldIVv\GWwdDDNZ4wuOSClbHXheoFo\Q>?	M{Do[VI1QTVzNEey

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	PARP / c-PARP / cleaved caspase 3 ; PubMed: 21393866 J Clin Invest H146 cells were preincubated in normoxia or hypoxia (1% O2) for 18 hours prior to treatment with ABT-737 (89.1 nM ), after which cells were harvested for protein analysis by Western blot. Hif-1a; PubMed: 22006676 Mol Cancer Ther Representative western blots for HIF-1α, PARP and cleaved caspase 3 in response to 24-72 hr exposure to ABT-737 in varying concentration in normoxia and hypoxia in 4 neuroblastoma cell lines. Actin is shown as a loading control. Blots are representative of 3 independent experiments. γ-H2AX / p-ATM; PubMed: 21084274 Cancer Res Induction of γ-H2AX and p-ATM by ABT-737. Cells were treated with 10 µmol/L ABT-737 for 24 hours and then maintained in fresh media for 1 or 2 more days prior to Western blot analysis.	21393866 22006676 21084274
Immunofluorescence	cytochrome C; PubMed: 26447615 Oncotarget Immunocytochemistry revealed the release of mitochondrial cytochrome c (green) into the cytoplasm after ABT-737 exposure (20 μM in MC-3 cells and 22.5 μM in HN22 cells) for 24 hr. MitoTracker (red) staining labels mitochondria within each field. Bax; PubMed: 26447615 Oncotarget Immunocytochemistry revealed the mitochondrial translocation of Bax from the cytoplasm after ABT-737 treatment (20 μM in MC-3 cells and 22.5 μM in HN22 cells) for 24 hr. MitoTracker (red) staining labels mitochondria within each field C. To assess whether ABT-737 treatment has an effect on the dimerization of Bax, the levels of dimeric Bax were measured with or without ABT-737 treatment in MC-3 and HN22 cells. Bim; PubMed: 26447615 Oncotarget Immunocytochemistry revealed the mitochondrial translocation of Bim from the cytoplasm after ABT-737 treatment (20 μM in MC-3 cells and 22.5 μM in HN22 cells) for 24 hr. MitoTracker (red) staining labels mitochondria within each field. AIF; PubMed: 25034785 Cell Death Differ localization of apoptosis inducing factor (AIF) in LCSC pre-stained with Mitotracker Red and untreated or treated with 500 nM ABT-737 for 48 h. Magnification × 60, zoom × 3, bar 20 μm. p65 ; PubMed: 28846096 Nat Cell Biol BCL-xL dependent SVEC cells were treated with ABT-737 (10 μM) +/- Q-VD-Oph (30 μM) for 1 h, immunostained for p65 and analysed by confocal microscopy. TNF (20 ng/ml) was used as positive control for p65 nuclear translocation. Scale bar represents 30μM. Representative images from three independent experiments.	26447615 25034785 28846096
Growth inhibition assay	Cell viability; PubMed: 22311987 J Biol Chem Stably transfected K562 cells were treated with increasing concentrations of ABT-737, obatoclax, or maritoclax for 24 h. Cell viability was determined by measuring intracellular ATP levels with the CellTiter Glo assay.	22311987
ELISA	IL-6 / IL-8; PubMed: 21084274 Cancer Res The secretion of IL-6 and IL-8 in PV-10 cells treated with DMSO, ABT-737 or enantiomer for 24 hours was determined by ELISA.	21084274

In vivo

In aggressive leukemia model, ABT-737 suppresses the leukemia burden by 53% at the 30 mg/kg, with significantly extended survival of mice. ABT-737 does not induce significantly abnormalities in blood cell counts or serum chemistries. ^[1] ABT-737 prolongs the survival of recipient mice transplanted with Bcl-2-transduced tumors. ^[2] ABT-737 shows great antitumor activity in an ATLL mouse model at a dose of 100 mg/kg. ^[5]

Protocol

Kinase Assay: ^[1]	- Collapse Fluorescence polarization assays: Binding affinity of GST-Bcl-2 family proteins to the FITC-conjugated BH3 domain of Bim (FITC-Ahx-DMRPEIWIAQELRRIGDEFNAYYAR) is determined. Briefly, 100 nM of GST-Bcl-2 family fusion proteins are incubated with serial dilutions of ABT-737 in PBS for 2 min. Then, 20 nM of FITC-Bim BH3 peptide (FITC-Ahx-DMRPEIWIAQELRRIGDEFNAYYAR) is added. Fluorescence polarization is measured using an Analyst TM AD Assay Detection System after 10 min using the 96-well black plate. Then IC50 are determined.
Cell Research: ^[4]	- Collapse Cell lines: SCLC cell lines NCI-H889, NCI-H1963, NCI-H1417, NCI-H146, NCI-187, DMS79, NCI-1048, NCI-H82, NCI-H196, H69AR, and DMS114 Concentrations: 0.001-10 μM Incubation Time: 48 hours Method: SCLC cells are treated for 48 hours in 96-well tissue culture plates in a total volume of 100 μL tissue culture medium supplemented with 10% human serum. Viable cells are determined using the MTS assay. (Only for Reference)
Animal Research: ^[1]	- Collapse Animal Models: Scid mice injected with Luc-expressing FD/ΔRaf-1:ER cells Formulation: 1 g/mL stock solution of ABT-737 in DMSO is added to a mixture of 30% propylene glycol, 5% Tween 80, 65% D5W (5% dextrose in water) (pH 4−5; final concentration of DMSO ≤ 1%) Dosages: 20 and 30 mg/kg Administration: For intraperitoneal (i.p.) every day (Only for Reference)

References

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Solubility (25°C)

In vitro	DMSO	100 mg/mL (122.93 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 30% Propylene glycol, 5% Tween 80, 65% D5W 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 ABT-737 SDF

Molecular Weight	813.43
Formula	C₄₂H₄₅ClN₆O₅S₂
CAS No.	852808-04-9
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	N/A
Smiles	CN(C)CCC(CSC1=CC=CC=C1)NC2=CC=C(C=C2[N+]([O-])=O)[S](=O)(=O)NC(=O)C3=CC=C(C=C3)N4CCN(CC4)CC5=C(C=CC=C5)C6=CC=C(Cl)C=C6

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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.

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Frequently Asked Questions

Question 1:
What’s the recommended method about reconstitution of the compound for in vivo animal study?
Answer:
For oral administration, we suggest the vehicle: 30% Propylene glycol, 5% Tween 80, 65% D5W, at up to 30mg/ml; For injection, ABT-737 can be dissolved in 2% DMSO/50% PEG 300/5% Tween 80/ddH2O at 2.5 mg/ml.

Bcl-2 Signaling Pathway Map

Bcl-2 Inhibitors with Unique Features

Selective Bcl-2 Inhibitor

ABT-199 (GDC-0199) : Bcl-2-selective, K_i<0.01 nM.
Most Potent Bcl-2 Inhibitor

ABT-263 (Navitoclax) : Bcl-xL, K_i≤ 0.5 nM; Bcl-2, K_i≤ 1 nM; Bcl-w, K_i≤ 1 nM.
Bcl-2 Inhibitor in Clinical Trial

Obatoclax Mesylate (GX15-070) : Phase II for leukemia, lymphoma, myelofibrosis, and mastocytosis.
Newest Bcl-2 Family Activator

BAM7 : Direct and selective activator of proapoptotic Bax with EC50 of 3.3 μM.

Related Bcl-2 Products

A-1210477 ^New

A-1210477 is a potent and selective MCL-1 inhibitor with K_i and IC50 of 0.454 nM and 26.2 nM, respectively, >100-fold selectivity over other Bcl-2 family members.
MI-773 (SAR405838) ^New

MI-773 (SAR405838) is an orally available MDM2 antagonist with K_i of 0.88 nM. Phase 1.
Navitoclax (ABT-263)

Navitoclax (ABT-263) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with K_i of ≤ 0.5 nM, ≤1 nM and ≤1 nM in cell-free assays, but binds more weakly to Mcl-1 and A1. Phase 2.
Venetoclax (ABT-199)

Venetoclax (ABT-199, GDC-0199) is a Bcl-2-selective inhibitor with K_i of <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Phase 3.

Features:Re-engineered version of ABT-263 (Navitoclax).
UMI-77

UMI-77 is a selective Mcl-1 inhibitor with Ki of 490 nM, showing selectivity over other members of Bcl-2 family.
Obatoclax Mesylate (GX15-070)

Obatoclax Mesylate (GX15-070) is an antagonist of Bcl-2 with K_i of 0.22 μM in a cell-free assay, can assist in overcoming MCL-1 mediated resistance to apoptosis. Phase 3.

Features:Potential 1st-in-class small molecule antagonist of Bcl-2 designed to inhibit all relevant Bcl-2 family members, including Mcl-1.
TW-37

TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with K_i of 0.29 μM, 1.11 μM and 0.26 μM in cell-free assays, respectively.
Sabutoclax

Sabutoclax(BI-97C1) is a pan-Bcl-2 inhibitor, including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively.
AT101

AT101, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with K_i of 0.32 μM, 0.48 μM and 0.18 μM in cell-free assays; does not inhibit BIR3 domain and BID. Phase 2.

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ABT-737