Tapotoclax 是一种针对诱导性髓系白血病细胞分化蛋白 MCL-1 的高效抑制剂 (Ki=0.13 nM),具备潜在的促凋亡和抗肿瘤活性。给药后,Tapotoclax 与 MCL-1 结合,从而抑制其功能。这一过程阻止了 MCL-1 与 Bcl-2 类蛋白 11 (BCL2L11;BIM) 的复合物形成,并进一步触发肿瘤细胞凋亡。 Tapotoclax is a potent inhibitor (Ki=0.13 nM) of the inducible myeloid leukemia cell differentiation protein MCL-1, with potential pro-apoptotic and anti-tumor activity. Upon administration, Tapotoclax binds to MCL-1, thereby inhibiting its function. This process prevents the formation of a complex between MCL-1 and Bcl-2-like protein 11 (BCL2L11; BIM) and further triggers apoptosis in tumor cells.
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Tapotoclax
CAS number:1883727-34-1 molecular formula:C33H41ClN2O5S
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| Chinese alias | 他普托克拉 | ||
| English alias | BCP25146 | AKOS040741103 | EX-A2666 | VF8 | AMG 176 [WHO-DD] | SR-05000001528-2 | AC-36265 | MCL-1 inhibitor AMG 176 | 97W7N9T08G | MS-30719 | (3'R,4S,6'R,7'S,8'E,11'S,12'R)-7-chloro-7'-methoxy-11',12'-dimethyl-13',13'-dioxospiro[2,3-dihydro-1H-naphthalen | ||
| CAS number | 1883727-34-1 | molecular formula | C33H41ClN2O5S |
| molecular weight | 613.21 g/mol | Exact mass | - |
| PSA | 93.300 Ų | logp | 6.800 |
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