CAN508

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Chemical Structure| 140651-18-9 同义名 : CAY10574
CAS号 : 140651-18-9
货号 : A1210582
分子式 : C9H10N6O
纯度 : 97%
分子量 : 218.215
MDL号 : MFCD09262258
存储条件:

Pure form Keep in dark place,Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 250 mg/mL(1145.66 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 CAN508 is a strong, ATP-competitive inhibitor of CDK9/cyclin T1, with an IC50 of 0.35 μM, showing 38 times more selectivity for CDK9/cyclin T compared to other CDK/cyclin complexes, and has demonstrated antitumor activity[1]. It decreases the proportion of S-phase cells in the HT-29 cancer cell line in antiproliferation assays[1]. At concentrations of 20-40 μM over 72 hours, CAN508 notably reduces cell proliferation in a dose-dependent manner across three esophageal adenocarcinoma cell lines (SKGT4, OE33, and FLO-1), with IC50 values ranging from 34.99 to 91.09 μM. Additionally, at 40 μM for 72 hours, CAN508 increases apoptosis in these esophageal adenocarcinoma cells[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.58mL

0.92mL

0.46mL

22.91mL

4.58mL

2.29mL

45.83mL

9.17mL

4.58mL

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.