Voruciclib |
| رقم الكتالوجGC45983 |
Voruciclib هو مثبط CDK نشط عن طريق الفم وانتقائي مع قيم Ki من 0.626 نانومتر -9.1 نانومتريحظر Voruciclib بشكل فعال CDK9 ، منظم النسخ لـ MCL-1يقوم Voruciclib بقمع التعبير عن MCL-1 في نماذج متعددة من سرطان الغدد الليمفاوية B- الخلية الكبيرة المنتشرة (DLBCL)
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Cas No.: 1000023-04-0
Sample solution is provided at 25 µL, 10mM.
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Voruciclib is a pan-inhibitor of cyclin-dependent kinases (CDKs; Kis = 0.626-9.1 nM).1 It is selective for CDKs over male germ cell associated kinase (MAK) and intestinal cell kinase (ICK; Kis = 259 and 481 nM, respectively), in a panel of 48 kinases. Voruciclib decreases myeloid cell leukemia-1 (Mcl-1) levels and increases cleaved poly(ADP-ribose) polymerase (PARP) levels in six diffuse large B-cell lymphoma (DLBCL) cell lines when used at concentrations ranging from 0.5 to 5 μM. It reduces tumor growth by 56.3% in a Ri-1 mouse xenograft model when administered at a dose of 200 mg/kg.
|1. Dey, J., Deckwerth, T.L., Kerwin, W.S., et al. Voruciclib, a clinical stage oral CDK9 inhibitor, represses MCL-1 and sensitizes high-risk diffuse large B-cell lymphoma to BCL2 inhibition. Sci. Rep. 7(1), 18007 (2017).
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