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首页-小分子抑制剂&激动剂-Apoptosis-Bcl-2-S-63845
S-63845

Chemical Structure : S-63845

CAS No.: 1799633-27-4

S-63845 (S 63845;S63845)

货号: PC-42244Not For Human Use, Lab Use Only.

S-63845 (S63845) is a highly potent, selective Mcl-1 inhibitor with Kd of 0.19 nM, with no appreciable binding affinity to BCL-2 or BCL-XL (Ki>10 uM).

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10 mg ¥3980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

S-63845 (S63845) is a highly potent, selective Mcl-1 inhibitor with Kd of 0.19 nM, with no appreciable binding affinity to BCL-2 or BCL-XL (Ki>10 uM).
S-63845 binds to the BH3-binding groove of Mcl-1.
S-63845 potently kills MCL1-dependent cancer cells, including multiple myeloma (IC50<0.1 uM), leukaemia and lymphoma cells, by activating the BAX/BAK-dependent mitochondrial apoptotic pathway.
S-63845 is well tolerated and shopws high effectivity against mouse cancer models.

物理化学性质&存储条件

分子量 829.2593
分子式 C39H37ClF4N6O6S
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

Chemical Name/SMILES

Dispiro[cyclohexane-1,2'-[2H]indene-1'(3'H),2''-[2H]imidazol]-4''-amine, 4-methoxy-5''-methyl-6'-[5-(1-propyn-1-yl)-3-pyridinyl]-, (1α,1'R,4β)-

参考文献

1. Kotschy A, et al. Nature. 2016 Oct 27;538(7626):477-482.

2. Merino D, et al. Sci Transl Med. 2017 Aug 2;9(401). pii: eaam7049.

3. Letai A. Cancer Cell. 2016 Dec 12;30(6):834-835.

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