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编 号:F142102
分子式:C21H22Cl2FN5O
分子量:450.34
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10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
(S)-Crizotinib is a potent and selective MTH1 (mutT homologue) inhibitor with an IC50 of 330 nM. (S)-Crizotinib disrupts nucleotide pool homeostasis via MTH1 inhibition, induces an increase in DNA single strand breaks, activates DNA repair in human colon carcinoma cells, and effectively suppresses tumour growth in animal models.

体内研究:
(S)-crizotinib (7.5 或 15 mg/kg;腹腔注射;每天一次,连续10天)可显着降低肿瘤体积和肿瘤重量。Animal Model:Five-week-old, athymic BALB/c nu/nu female mice (17-19 g) with NCI-H460 cells
Dosage:7.5 or 15 mg/kg
Administration:Intraperitoneal injections; once daily for 10 days
Result:Resulted in significant reductions in both tumor volume and tumor weight.

体外研究:
(S)-crizotinib (0.625-80 μM; 24 hours) 降低了 NCI-H460,H1975 和 A549 细胞的活力,IC50 值分别为 14.29、16.54 和 11.25 μM。(S)-crizotinib (10-30 μM; 24 hours) 诱导 NCI-H460,H1975 和 A549 细胞凋亡。 (S)-crizotinib (10-30 μM; 24 hour
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