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首页-小分子抑制剂&激动剂-Apoptosis-Bcl-2-A-1331852
A-1331852

Chemical Structure : A-1331852

CAS No.: 1430844-80-6

A-1331852 (A1331852, A 1331852)

货号: PC-45700Not For Human Use, Lab Use Only.

A-1331852 (A1331852) is a potent and selective BCL-XL inhibitor (Ki<10 pM).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

A-1331852 (A1331852) is a potent and selective BCL-XL inhibitor (Ki<10 pM).
A-1331852 shows much weaker affinity for BCL-2 (Ki=6 nM), BCL-W (Ki=4 nM), and MCL-1 (Ki=142 nM).
A-1331852 selectively disrupts BCL-XL–BIM complexes and induces the hallmarks of apoptosis in BCL-XL–dependent Molt-4 cells (Molt-4 viability IC50=6 nM).
A-1331852 demonstrates antitumor efficacy in the Molt-4 xenograft model; orally active.

物理化学性质&存储条件

分子量 658.8117
分子式 C38H38N6O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 12 mg/mL

Chemical Name/SMILES

2-Pyridinecarboxylic acid, 6-[8-[(2-benzothiazolylamino)carbonyl]-3,4-dihydro-2(1H)-isoquinolinyl]-3-[5-methyl-1-(tricyclo[3.3.1.13,7]dec-1-ylmethyl)-1H-pyrazol-4-yl]-

参考文献

1. Leverson JD, et al. Sci Transl Med. 2015 Mar 18;7(279):279ra40.

2. Punnoose EA, et al. Mol Cancer Ther. 2016 May;15(5):1132-44.

3. Lucas CM, et al. Leukemia. 2016 Jun;30(6):1273-81.

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