CP-10 is a PROTAC connected by ligands for Cereblon and CDK, with highly selective, specific, and remarkable CDK6 degradation (DC 50 =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.
性状
Solid
IC50 & Target[1][2]
CDK6 2.1 nM (DC50) Cereblon
体外研究(In Vitro)
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).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). has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
参考文献
[1]. Su S, et al. Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders. J Med Chem. 2019 Aug 2.
溶解度数据
In Vitro: DMSO : 200 mg/mL (229.37 mM; Need ultrasonic)配制储备液