CAY10574

CAY10574

中文名称CAY10574
中文同义词化合物CAN508;4-((3,5-二氨基-1H-吡唑-4-基)偶氮基)苯酚
英文名称CAY10574
英文同义词CAY10574;Cdk9 Inhibitor II;4-[2-(3,5-diamino-1H-pyrazol-4-yl)diazen-1-yl]phenol;CAN-508;CAN-508 (CAN508);CaMKII Inhibitor, CK59 - CAS 140651-18-9 - Calbiochem;inhibit,CAN 508,ATP-competitive,Cyclin dependent kinase,esophageal,cells,CDK,CAN508,Inhibitor,adenocarcinoma,HT-29,CAN-508;Phenol, 4-[2-(3,5-diamino-1H-pyrazol-4-yl)diazenyl]-
CAS号140651-18-9
分子式C9H10N6O
分子量218.22
EINECS号
相关类别
Mol文件140651-18-9.mol
结构式CAY10574 结构式

CAY10574 性质

沸点638.3±55.0 °C(Predicted)
密度1.67±0.1 g/cm3(Predicted)
储存条件+2C to +8C
溶解度DMF:0.5mg/mL;二甲基亚砜:0.5mg/mL
酸度系数(pKa)8.52±0.30(Predicted)
形态黄色半固体
颜色浅黄至黄色

CAY10574 用途与合成方法

CAN508 是一种有效的、ATP 竞争性抑制 CDK9/cyclin T1,IC50为 0.35 μM。CAN508 对 CDK9/cyclin T1 比对其他的 CDK/cyclin 高出 38 倍的选择性。CAN508 具有抗肿瘤活性。

CDK9/cyclinT1

0.35 μM (IC 50 )

CDK2/cyclinE

20 μM (IC 50 )

cdk2/cyclin A

69 μM (IC 50 )

Cdk4/cyclin D1

13.5 μM (IC 50 )

CDK7/cyclin H

26 μM (IC 50 )

Cdk1/cyclin B

44 μM (IC 50 )

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 IC 50 s ranging from 34.99 to 91.09 μM.
CAN508 (40 μM; 72 hours) increases apoptosis in all three esophageal adenocarcinoma cells.

Apoptosis Analysis

Cell Line: SKGT4, OE33 and FLO-1 cells
Concentration: 40 μM
Incubation Time: 72 hours
Result: Increased apoptosis by 2 fold in all three esophageal adenocarcinoma cells compared to untreated controls.

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.

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/08/19HY-100429CAN5081 mg300元
2024/08/19HY-100429CAY10574
CAN508
140651-18-95mg600元

CAY10574 上下游产品信息

"CAY10574"相关产品信息
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