CAY10574

生物活性靶点体外研究体内研究 CAY10574 试剂级价格

CAY10574

CAS号:140651-18-9
英文名:CAY10574
中文名:CAY10574
CBNumber:CB62590428
分子式:C9H10N6O
分子量:218.22
MOL File:140651-18-9.mol

CAY10574化学性质

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: 0.5 mg/ml; DMSO: 0.5 mg/ml
酸度系数(pKa) :8.52±0.30(Predicted)
形态 :Yellow semi-solid
颜色 :Light yellow to yellow

CAY10574性质、用途与生产工艺

生物活性 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。

靶点

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 )

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 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.

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.