货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
V54136-1ml	10mM in DMSO	￥320.00 V54136-1ml ￥320.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

V54136-1ml

10mM in DMSO

￥320.00

货期：3-5天

产品描述：

CAN508 is a potent, ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. Antitumor activity

靶点：

CDK9/cyclinT1：0.35 μM (IC50)；CDK2/cyclinE：20 μM (IC50)；cdk2/cyclin A：69 μM (IC50)；Cdk4/cyclin D1：13.5 μM (IC50)；CDK7/cyclin H：26 μM (IC50)；Cdk1/cyclin B：44 μM (IC50);CDK

体外研究：

CAN508 reduces the frequency of S-phase cells of the cancer cell line HT-29 in antiproliferation assays.

CAN508 (20-40 μM; 72 hours) significantly reduces cell proliferation in a dose dependent manner in all three esophageal adenocarcinoma cell lines (SKGT4, OE33 and FLO-1 cells) with IC50s ranging from 34.99 to 91.09 μM.

CAN508 (40 μM; 72 hours) increases apoptosis in all three esophageal adenocarcinoma cells.

体内研究：

CAN508 (60 mg/kg; i.p.; daily for 10 days) has antitumor effects in esophageal adenocarcinoma xenografts. Animal Model: 4 weeks-old female nude mice (esophageal adenocarcinoma xenografts) Dosage: 60 mg/kg Administration: I.p.; daily for 10 days Result: Caused reduction of tumor growth starting from post-treatment day three with 50.83% reduction.

参考文献：

1. Krystof V, et al. 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. J Med Chem. 2006;49(22):6500-6509.

2. Tong Z, et al. Antitumor effects of cyclin dependent kinase 9 inhibition in esophageal adenocarcinoma. Oncotarget. 2017;8(17):28696-28710.

溶解性：

Soluble in DMSO

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	4.583 ml	22.913 ml	45.825 ml
5 mM	0.917 ml	4.583 ml	9.165 ml
10 mM	0.458 ml	2.291 ml	4.583 ml
50 mM	0.092 ml	0.458 ml	0.917 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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