产品
编 号:F341078
分子式:C13H11N3O2
分子量:241.25
产品类型
结构图
CAS No: 377090-84-1
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产品详情
生物活性:
SU9516 is a potent CDK2 inhibitor, with an IC50 of 22 nM, and also shows inhibitory effects on CDK1 and CDK4, with IC50s of 40, 200 nM, respectively.
体外研究:
SU9516 shows slight activities against PKC, p38, PDGFr and EGFR, with IC50 of >10, >10, 18, and >100 μM. SU9516 (5 μM) decreases cdk2-specific Phosphorylation of pRB and inhibits cell cycle progression in RKO cells. SU9516 (5 μM) also induces apoptosis in RKO and SW480 Cells. SU9516 (5 μM) results in enhanced pRb/E2F complex formation in HT-29 cells. SU9516 enhances presence of E2F species in multiprotein complexes. SU9516 (5 μM) rapidly induces cytochrome crelease, Bax mitochondrial translocation, and apoptosis in association with pronounced down-regulation of the antiapoptotic protein Mcl-1. SU9516 causes down-regulation of Mcl-1 mRNA levels in human leukemia cells. Furthermore, SU9516 treatment results in a marked increase in reactive oxygen species production.