货号	规格	价格	上海	北京	珠海	重庆	武汉
S81469-5mg促销	99.90%	￥100.00 ￥80.00 S81469-5mg ￥80.00 现货	9 9	-	-	-	-
S81469-10mg促销	99.90%	￥180.00 ￥144.00 S81469-10mg ￥144.00 现货	9 9	-	-	-	-
S81469-50mg促销	99.90%	￥590.00 ￥472.00 S81469-50mg ￥472.00 现货	6 6	-	-	-	-

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产品描述：

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.

靶点：

CDK2:22 nM (IC50);CDK1:40 nM (IC50);CDK4:200 nM (IC50);PDGFr:18000 nM (IC50);Apoptosis; p38MAPK; CDK; PKC; Autophagy

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

参考文献：

1. Lane ME, et al. A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells. Cancer Res. 2001 Aug 15;61(16):6170-7. 2. Yu B, et al. SU9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight E2F complexes in human colon carcinoma cells. Biochem Pharmacol. 2002 Oct 1;64(7):1091-100. 3. Gao N, et al. The three-substituted indolinone cyclin-dependent kinase 2 inhibitor 3-[1-(3H-imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one (SU9516) kills human leukemia cells via down-regulation of Mcl-1 through a transcriptional mechanism. Mol Pharmacol. 2006 Aug;70(2):645-55.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	4.145 ml	20.726 ml	41.452 ml
5 mM	0.829 ml	4.145 ml	8.29 ml
10 mM	0.415 ml	2.073 ml	4.145 ml
50 mM	0.083 ml	0.415 ml	0.829 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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