CP-10 是具有高选择性，特异性和显著的 CDK6 降解潜力 (DC50=2.1 nM) 的 PROTAC。它抑制几种造血细胞癌的增殖，包括多发性骨髓瘤，并且对突变和过表达的 CDK6 仍然可以降解。
CP-10 is a PROTAC with highly selective, specific, and remarkable CDK6 degradation (DC50=2.1 nM). It inhibits proliferation of several haematopoietic cancer cells with impressive potency including multiple myeloma, and can still degrades mutated and overexpressed CDK6[1]. CDK6|2.1 nM (DC50)
CP-10 induces nearly 72% degradation of CDK6 at 10 nM and 89% at 100 nM in human glioblastoma U251 cells. The degradation of CDK4 induced by CP-10 is far weaker than that of CDK6 (DC50: 50-80 fold)[1].CP-10 displays a cell inhibition potential in multiple myeloma cell MM.1S (IC50≈10 nM) and mantle cell lymphoma cells (in Mino, IC50≈8 nM)[1].
[1]. Su S, et al. Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders. J Med Chem. 2019 Aug 2.
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