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抑制剂 > DNA损伤/DNA修复 > CCT244747
产品名称:
CCT244747
型号:
CS-01Y70340
生产地址
进口、国产
产品价格
电议
产品简介
质量保证、价格优惠
产品详情

一、概述:

化学性质:                                                                                                             

规格

5mg 25mg

CAS

1404095-34-6

别名

 

化学名

(R)-3-((1-(dimethylamino)propan-2-yl)oxy)-5-((4-methoxy-5-(1-methyl-1H-pyrazol-4-yl)pyridin-2-yl)amino)pyrazine-2-carbonitrile

分子式

C20H24N8O2

分子量

408.46

溶解度

Soluble in DMSO

储存条件

Store at -20°C

General tips

For obtaining a higher solubility , please warm the tube at 37 and shake it in the ultrasonic bath for a while.

Shipping Condition

Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

 

产品描述:                                                                                                            

Description:

IC50: 29-170 nM

CHK1 is a serine/threonine kinase that is activated in response to single strand breaks (SSBs) in DNA caused by either direct DNA damage or replication stress. Activation of CHK1 initiates a signaling cascade culminating in cell cycle arrest leading to DNA repair, senescence or death. Inhibition of CHK1 abrogates cell cycle arrest, inhibits DNA repair and induces tumor cell death following DNA damage by a range of chemotherapeutic agents. CCT244747 is a potent and selective CHK1 inhibitor.

In vitro: CCT244747 inhibited cellular CHK1 activity, significantly enhanced the cytotoxicity of a few anticancer drugs and abrogated drug-induced S and G2 arrest in multiple tumor cell lines. Biomarkers of CHK1 activity and cell cycle inactivity were induced by genotoxics and inhibited by CCT244747, producing enhanced DNA damage and apoptosis [1].

In vivo: Active tumor concentrations of CCT244747 were obtained following oral administration. The antitumor activities of both gemcitabine and irinotecan were significantly enhanced by CCT244747 in human tumor xenografts, giving concomitant biomarker modulation indicative of CHK1 inhibition [1].

Clinical trial: Up to now, CCT244747 is still in the preclinical development stage.

特别提醒:                                                                                                              

1. 本产品仅供科研使用。请勿用于医药、临床诊断或治疗,食品及化妆品等用途。请勿存放于普通住宅区。

2. 为了您的安全和健康,请穿好实验服并佩戴一次性手套和口罩操作。

标签:CCT244747 

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