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Information S63845 S63845 is a new, selective MCL-1 inhibitor with the Kd value of 0.19 nM and has no discernible binding to the other BCL-2 members, BCL-2 or BCL-XL. Targets human MCL-1 0.19 nM(Kd) In vitro S63845 induces death of cancer cell lines with known reliance on MCL-1, displaying classical hallmarks of apoptosis that are dependent on caspases and BAX/BAK-mediated mitochondrial outer membrane permeabilisation. It has a 6 fold higher affinity for human MCL-1 over mouse MCL-1. S63845 is effective against haematological cancer-derived cell lines in vitro and in vivo and also AML samples, but does not readily kill normal human haematopoietic progenitor cells. In vivo S63845 shows potent anti-tumour activity with an acceptable safety margin as a single agent in several cancers. S63845 is well tolerated by the mice with no significant weight loss observed. Some of solid tumour models shows sensitivity to S63845 monotherapy, while many others are only killed when treated with a combination of S63845 and inhibitors of oncogenic kinases. Cell Research(from reference) Cell lines:HeLa cells Concentrations:0.1, 0.3, 1, 3 μM Incubation Time:4 h
中文名称
S63845
英文名称
S63845
中文别名
-
英文别名
Benzenepropanoic acid,α-​[[(5S)​-​5-​[3-​chloro-​2-​methyl-​4-​[2-​(4-​methyl-​1-​piperazinyl)​ethoxy]​phenyl]​-​6-​(5-​fluoro-​2-​furanyl)​thieno[2,​3-​d]​pyrimidin-​4-​yl]​oxy]​-​2-​[[1-​(2,​2,​2-​trifluoroethyl)​-​1H-​pyrazol-​5-​yl]​methoxy]​-​,(αR)
CAS号
1799633-27-4
分子式
C39H37ClF4N6O6S
分子量
829.26 g/mol
精确质量
≥99%
PSA
156.000 Ų
Logp
5.700
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MedMol S63845 99% 1mg

品牌:MedMol
货号:S84014-1mg
级别: -
货期:30天
已售 227 件
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