Chk1-IN-5

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Chk1-IN-5 

Chk1-IN-5 是有效的检查点激酶 1 (Chk1) 抑制剂。Chk1-IN-5 抑制 Chk1 磷酸化,并在结肠癌异种移植模型中抑制肿瘤生长。

Chk1-IN-5

Chk1-IN-5 Chemical Structure

CAS No. : 2120398-39-0

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生物活性

Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model[1].

IC50 & Target[1]

Chk1

 

体外研究
(In Vitro)

Chk1-IN-5 (compound 3; 0.4, 1.2, 3.7, 11.1, 33.3, 100 nM) inhibits Chk1 phosphorylation in the HT-29 colon cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Chk1-IN-5 (compound 3; 40 mg/kg; IV; twice a week for 21 days) inhibits tumor growth in Baib/c nude mice with HT-29 colon cancer cells[1].
Chk1-IN-5 (10 mg/kg; via tail vein intravenous injection) displays a longer half-life (T1/2=3.8 hours) and higher exposure (CL=2.3 L/hr•kg; Vss=6.4 L/kg; AUC=4531 ng/ml•h)[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Baib/c nude mice with HT-29 colon cancer cells[1]
Dosage: 40 mg/kg
Administration: IV; twice a week for 21 days
Result: Inhibited tumor growth.
Animal Model: Male SD rats (280-350 g)[1]
Dosage: 10 mg/kg
Administration: Via tail vein intravenous injection
Result: Displayed a longer half-life (T1/2=3.8 hours) and higher exposure (CL=2.3 L/hr•kg; Vss=6.4 L/kg; AUC=4531 ng/ml•h).

分子量

383.38

Formula

C18H18FN7O2

CAS 号

2120398-39-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Xiong Cai, et al. 3,5-disubstituted pyrazoles useful as checkpoint kinase 1 (chk1) inhibitors, and their preparations and applications. WO2017132928A1.

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