A-1155463

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    WARNING: This product is for research use only, not for human or veterinary use.

Description: A-1155463 is a highly potent and selective BCL-XL inhibitor. A-1155463 is substantially more potent against BCL-XL-dependent cell lines relative to WEHI-539, while possessing none of its inherent pharmaceutical liabilities. A-1155463 caused a mechanism-based and reversible thrombocytopenia in mice and inhibited H146 small cell lung cancer xenograft tumor growth in vivo following multiple doses. A-1155463 thus represents an excellent tool molecule for studying BCL-XL biology as well as a productive lead structure for further optimization.

Price and Availability

A-1155463, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

Synonym: A-1155463; A 1155463; A1155463.

IUPAC/Chemical Name: 2-(8-(benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1H)-yl)-5-(3-(4-(3-(dimethylamino)prop-1-yn-1-yl)-2-fluorophenoxy)propyl)thiazole-4-carboxylic acid

InChi Key: SOYCFODXNRVBTI-UHFFFAOYSA-N

InChi Code: InChI=1S/C35H32FN5O4S2/c1-40(2)17-6-8-22-14-15-28(26(36)20-22)45-19-7-13-30-31(33(43)44)38-35(47-30)41-18-16-23-9-5-10-24(25(23)21-41)32(42)39-34-37-27-11-3-4-12-29(27)46-34/h3-5,9-12,14-15,20H,7,13,16-19,21H2,1-2H3,(H,43,44)(H,37,39,42)

SMILES Code: O=C(C1=C(CCCOC2=CC=C(C#CCN(C)C)C=C2F)SC(N3CC4=C(C=CC=C4C(NC5=NC6=CC=CC=C6S5)=O)CC3)=N1)O

Technical Data

References

1: Zhang H, Xue J, Hessler P, Tahir SK, Chen J, Jin S, Souers AJ, Leverson JD,
Lam LT. Genomic analysis and selective small molecule inhibition identifies
BCL-X(L) as a critical survival factor in a subset of colorectal cancer. Mol
Cancer. 2015 Jul 2;14:126. doi: 10.1186/s12943-015-0397-y. PubMed PMID: 26134786;
PubMed Central PMCID: PMC4487849.

2: Leverson JD, Phillips DC, Mitten MJ, Boghaert ER, Diaz D, Tahir SK, Belmont
LD, Nimmer P, Xiao Y, Ma XM, Lowes KN, Kovar P, Chen J, Jin S, Smith M, Xue J,
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Tao ZF, Wendt MD, Sampath D, Rosenberg SH, Tse C, Huang DC, Fairbrother WJ,
Elmore SW, Souers AJ. Exploiting selective BCL-2 family inhibitors to dissect
cell survival dependencies and define improved strategies for cancer therapy. Sci
Transl Med. 2015 Mar 18;7(279):279ra40. doi: 10.1126/scitranslmed.aaa4642. PubMed
PMID: 25787766.

3: Tao ZF, Hasvold L, Wang L, Wang X, Petros AM, Park CH, Boghaert ER, Catron ND,
Chen J, Colman PM, Czabotar PE, Deshayes K, Fairbrother WJ, Flygare JA, Hymowitz
SG, Jin S, Judge RA, Koehler MF, Kovar PJ, Lessene G, Mitten MJ, Ndubaku CO,
Nimmer P, Purkey HE, Oleksijew A, Phillips DC, Sleebs BE, Smith BJ, Smith ML,
Tahir SK, Watson KG, Xiao Y, Xue J, Zhang H, Zobel K, Rosenberg SH, Tse C,
Leverson JD, Elmore SW, Souers AJ. Discovery of a Potent and Selective BCL-XL
Inhibitor with in Vivo Activity. ACS Med Chem Lett. 2014 Aug 26;5(10):1088-93.
doi: 10.1021/ml5001867. eCollection 2014 Oct 9. PubMed PMID: 25313317; PubMed
Central PMCID: PMC4190639.