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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-DNA Repair Protein -(S)-Crizotinib
(S)-Crizotinib

Chemical Structure : (S)-Crizotinib

CAS No.: 1374356-45-2

(S)-Crizotinib

货号: PC-27895Not For Human Use, Lab Use Only.

(S)-Crizotinib is a potent inhibitor of 7,8-dihydro-8-oxoguanine triphosphatase MTH1 (NUDT1) with IC50 of 72 nM and ITC KD of 47 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

(S)-Crizotinib is a potent inhibitor of 7,8-dihydro-8-oxoguanine triphosphatase MTH1 (NUDT1) with IC50 of 72 nM and ITC KD of 47 nM.
(S)-Crizotinib has IC50 of 330 nM and 408 nM for MTH1 substrates 8-oxo-dGTP and 2-OH-dATP, respectively.
(S)-Crizotinib efficiently inhibits colony formation of SW480 and KRAS mutated PANC1 cells, similar to SCH51344.
(S)-Crizotinib efficiently stabilized MTH1 validating the differential targeting within cells.
(S)-Crizotinib induced DNA damage in cancer cells and reduced tumour growth in SW480 colon carcinoma xenograft model.

物理化学性质&存储条件

分子量 450.34
分子式 C21H22Cl2FN5O
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

10 mM in DMSO

Chemical Name/SMILES

(S)-3-(1-(2,6-Dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine

参考文献

1. Huber KV, et al. Nature. 2014 Apr 10;508(7495):222-7.

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