CP-10 |
| رقم الكتالوجGC35739 |
CP-10 عبارة عن PROTAC متصل بواسطة روابط لـ Cereblon و CDK ، مع تدهور CDK6 انتقائي للغاية ومحدّد ورائع (DC50 = 2.1 نانومتر)يمنع تكاثر العديد من الخلايا السرطانية المكونة للدم بفاعلية مذهلة بما في ذلك المايلوما المتعددة ، ولا يزال بإمكانه تحطيم CDK6 المتحور والمفرط في التعبير
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Cas No.: 2366268-80-4
Sample solution is provided at 25 µL, 10mM.
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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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