1235034-55-5

1235034-55-5 structure

Name: A-1155463
Chemical Name: 2-[8-(1,3-Benzothiazol-2-ylcarbamoyl)-3,4-dihydro-2(1H)-isoquinolinyl]-5-(3-{4-[3-(dimethylamino)-1-propyn-1-yl]-2-fluorophenoxy}propyl)-1,3-thiazole-4-carboxylic acid
CAS Number: 1235034-55-5
Molecular Formula: C₃₅H₃₂FN₅O₄S₂
Molecular Weight: 669.788
Catalog: Signaling Pathways Apoptosis Bcl-2 Family
Create Date: 2018-04-28 05:23:58
Modify Date: 2024-01-10 10:48:27
A-1155463 is a highly potent and selective BCL-XL inhibitor with an EC50 of 70 nM in Molt-4 cell.

Name	2-[8-(1,3-Benzothiazol-2-ylcarbamoyl)-3,4-dihydro-2(1H)-isoquinolinyl]-5-(3-{4-[3-(dimethylamino)-1-propyn-1-yl]-2-fluorophenoxy}propyl)-1,3-thiazole-4-carboxylic acid
Synonyms	2-[8-(1,3-Benzothiazol-2-ylcarbamoyl)-3,4-dihydro-2(1H)-isoquinolinyl]-5-(3-{4-[3-(dimethylamino)-1-propyn-1-yl]-2-fluorophenoxy}propyl)-1,3-thiazole-4-carboxylic acid 4-Thiazolecarboxylic acid, 2-[8-[(2-benzothiazolylamino)carbonyl]-3,4-dihydro-2(1H)-isoquinolinyl]-5-[3-[4-[3-(dimethylamino)-1-propyn-1-yl]-2-fluorophenoxy]propyl]- A1155463 A-1155463

Description	A-1155463 is a highly potent and selective BCL-XL inhibitor with an EC50 of 70 nM in Molt-4 cell.
Related Catalog	Signaling Pathways >> Apoptosis >> Bcl-2 Family Research Areas >> Cancer
Target	Bcl-xL:0.01 nM (Ki) Bcl-2:80 nM (Ki)
In Vitro	A-1155463 shows picomolar binding affinity to BCL-XL (Ki＜0.01 nM), and >1000-fold weaker binding to BCL-2 (Ki= 80 nM) and related proteins BCL-W (Ki= 19 nM) and MCL-1 (Ki> 440 nM) [2]. A-1155463 demonstrates strong growth inhibition of over half of the colorectal cell lines as defined by EC50 values ≤0.5 μM in the presence of 10 % FBS[3].
In Vivo	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[2].
Animal Admin	Mice: Following a single 5 mg/kg IP dose of A-1155463 in nontumor bearing SCID-Beige mice, platelet counts fell dramatically as measured at 6 h postdose and then rebounded to normal levels within 72 h. A-1155463 is then administered to SCID-Beige mice that had been inoculated with BCL-XL-dependent H146 tumor cells with a daily dose at 5 mg/kg IP for 14 days[2].
References	[1]. Leverson JD, et al. 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):279 [2]. Tao ZF, et al. Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity. ACS Med Chem Lett. 2014 Aug 26;5(10):1088-93. [3]. Zhang H, et al. 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.

Density	1.5±0.1 g/cm3
Molecular Formula	C₃₅H₃₂FN₅O₄S₂
Molecular Weight	669.788
Exact Mass	669.187988
LogP	6.61
Index of Refraction	1.716
Storage condition	-20℃

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