CHIR-124,CHIR-124
  • CHIR-124,CHIR-124

405168-58-3CHIR-124

价格 询价
包装 1盒
最小起订量 1盒
发货地 上海
更新日期 2024-12-04
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产品详情

中文名称:CHIR-124英文名称:CHIR-124
CAS:405168-58-3品牌: 一研
保存条件: Store at -20°C产品类别: 抑制剂
Cas : 405168-58-3
2024-12-04 CHIR-124 CHIR-124 1盒/RMB 一研 Store at -20°C 抑制剂

产品属性:

产品名称

规格

CAS

型号

CHIR-124

10mM (in 1mL DMSO) 5mg 25mg 50mg

405168-58-3

EY-Y0165522

Cas No.405168-58-3

别名

化学名 4-[[(3S)-1-azabicyclo[2.2.2]octan-3-yl]amino]-6-chloro-3-(1,3-dihydrobenzimidazol-2-ylidene)quinolin-2-one

分子式 C23H22ClN5O

CHIR-124.png

分子量 419.91

溶解度 10.5mg/mL 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:
CHIR-124 abrogates the S and G2-M checkpoints induced by topoisomerase I poisons and selectively sensitizes tumors lacking p53 function to undergo mitotic death. In addition, CHIR-124 enhances the antitumor effect of irinotecan in tumor xenografts by inhibiting the G2-M checkpoint and inducing apoptosis.

In vitro, the effect of a matrix of camptothecin and CHIR-124 combinations in a number of human cancer cell lines, including breast carcinoma (MDA-MB-231and MDAMB-435) and colon carcinoma (SW-620 and Colo205), all of which are mutant for p53. When cells were simultaneously exposed to a matrix of different concentration combinations of CHIR-124 and SN-38 for 48 h, significant synergy or >10% deviation from additivity was observed in the concentration ranges of 4.2×108 mol/L for SN-38 and 6.0×108 mol/L for CHIR-124. Compared to IR alone, the number of mitotic cells increased dramatically in p53-/- HCT116 cells after concomitant Chir-124 exposure, while no such effect was observed in p53-sufficient WT HCT116 cells. Chir-124 was able to radiosensitize HCT116 cells that lack checkpoint kinase-2 (CHK2) or that were deficient for the spindle checkpoint protein Mad2. Additionally, Chir-124 could radiosensitize tetraploid cell lines, which were resistant to DNA damaging agents. Radiosensitization mediated by Chir-124 is greatly influenced by the p53 and cell cycle checkpoint system [1, 2].

In vivo, severe combined immunodeficient mice harboring MDA-MD-435 tumor xenografts were randomized into the treatment of 10 mg/kg CHIR-124, 20 mg/kg CHIR-124, 10 mg/kg CHIR-124 with 5 mg/kg CPT-11, or 20 mg/kg CHIR-124 with 5 mg/kg CPT-11. CPT-11 was given i.p. four times daily ×5 on days 1 to 5, while CHIR-124 was given orally four times daily ×6 on days 2 to 7 in captisol. Tumors harvested from mice sacrificed on day 4 of treatment were examined for apoptosis by terminal deoxynucleotidyl transferase-mediated nick-end labeling staining and for mitotic index by immunofluorescence labeling with phospho-histone H3 antibody in a similar study [1].

References:

[1]. Tse AN, Rendahl KG, Sheikh T, et al. CHIR-124, a novel potent inhibitor of Chk1, potentiates the cytotoxicity of topoisomerase I poisons in vitro and in vivo. Clinical Cancer Research, 2007, 13(2): 591-602.

[2]. Tao YG, Leteur C, Yang CY, et al. Radiosensitization by Chir-124, a selective CHK1 inhibitor Effects of p53 and cell cycle checkpoints. Cell Cycle, 2007, 8(8): 1196-1205.


关键字: 405168-58-3;C23H22ClN5O;CHIR-124;

公司简介

上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要从事免疫学、分子生物学和常规生化试剂等为一体的科研产品销售企业,公司自成立以来,秉承""全心全意服务于科研工作者""的企业理念,立足生物科技领域,运用生物技术和科研试剂,发展现代生物科技,为各类大中小医院及其它医疗机构、高等院校、科研院所、企事业单位提供优质的产品,服务生物科技领域的科学研究人员。 公司具有对普通货物、冷藏及冷冻仓库的存储、包装及运输能力。 公司将始终坚持信誉立业、以人为本、质量保证、诚信服务的宗旨,不断拼搏,开拓进取,与各界朋友携手共创美好未来。
成立日期 2014-06-05 (11年) 注册资本 100
员工人数 50-100人 年营业额 ¥ 100万以内
主营行业 生化试剂,抗体,细胞培养,分子生物学,免疫安全 经营模式 工厂,试剂
  • 上海一研生物科技有限公司
VIP 3年
  • 公司成立:11年
  • 注册资本:100
  • 企业类型:营业执照
  • 主营产品:、ELISA试剂盒、PCR检测试剂盒、生化检测试剂盒、标准品、抗体、细胞等
  • 公司地址:上海市闵行区莘福路2号楼
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