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
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S63845
CAS number：1799633-27-4 molecular formula：C39H37ClF4N6O6S
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| Chinese alias | - | ||
| English alias | 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 number | 1799633-27-4 | molecular formula | C39H37ClF4N6O6S |
| molecular weight | 829.26 g/mol | Exact mass | ≥99% |
| PSA | 156.000 Ų | logp | 5.700 |
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