A-1155463

Research use only, not for human use.

A-1155463 is a highly potent and selective BCL-XL inhibitor (Ki=10 pM).

A-1155463 is a highly potent and selective BCL-XL inhibitor (Ki=10 pM); shows >1000-fold weaker binding to BCL-2, BCL-W (Ki =19 nM) and MCL-1 (Ki >440 nM); inhibits H146 SCLC xenograft tumor growth in vivo.(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) . 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.(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.

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A1155463 | A 1155463

Angiogenesis

Bcl-2

Bcl-xL|Bcl-2

Cancer

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1235034-55-5

669.7881

C35H32FN5O4S2

>98% (HPLC)

DMSO: ≥ 31 mg/mL

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

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]-

(-20℃)

With Ice Pack

≥ 2 years