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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Checkpoint Kinase (Chk)-CHIR-124
CHIR-124

Chemical Structure : CHIR-124

CAS No.: 405168-58-3

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CHIR-124 (CHIR124, CHIR 124)

货号: PC-43443Not For Human Use, Lab Use Only.

CHIR-124 is a potent, selective Chk1 inhibitor with in vitro IC50 of 0.3 nM, 2,000-fold selectivity over Chk2.

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10 mg ￥1280 In stock
25 mg ￥1980 In stock
50 mg ￥3280 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CHIR-124 is a potent, selective Chk1 inhibitor with in vitro IC50 of 0.3 nM, 2,000-fold selectivity over Chk2.
CHIR-124 displays 500- to 5,000-fold less active against other cell cycle kinases, such as CDK2/cyclin A , Cdc2/cyclin B, and CDK4/cyclin D.
CHIR-124 also potently inhibits PDGFR and FLT3 with IC50s of 6.6 nM and 5.8 nM.
CHIR-124 interacts synergistically with topoisomerase poisons (e.g., camptothecin or SN-38) in causing growth inhibition in several p53-mutant solid tumor cell lines, abrogates the SN-38-induced S and G2-M checkpoints and potentiates apoptosis in MDA-MD-435 breast cancer cells, also restores the level of cdc25A protein.
CHIR-124 potentiates the growth inhibitory effects of irinotecan in breast cancer xenograft models.

物理化学性质&存储条件

分子量 419.91
分子式 C23H22ClN5O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: 14 mg/mL
Chemical Name/SMILES

2(1H)-Quinolinone, 4-[(3S)-1-azabicyclo[2.2.2]oct-3-ylamino]-3-(1H-benzimidazol-2-yl)-6-chloro-

参考文献

1. Tse AN, et al. Clin Cancer Res. 2007 Jan 15;13(2 Pt 1):591-602.

2. Tao Y, et al. Cell Cycle. 2009 Apr 15;8(8):1196-205.

3. Lee JH, et al. Proc Natl Acad Sci U S A. 2011 Dec 6;108(49):19629-34.

4. Seiler JA, et al. Mol Cell Biol. 2007 Aug;27(16):5806-18.

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