产品
编 号:F245496
分子式:C25H22ClF3N4O2
分子量:502.92
产品类型
结构图
CAS No: 1979939-16-6
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产品详情
生物活性:
CRT0273750 is an autotaxin (ATX) inhibitor and modulates LPA levels in plasm (IC50 = 0.014 μM). CRT0273750 can be used in ATX/LPA-dependent models of cancer.
体内研究:
CRT0273750 (1 mg/kg;iv) 具有中等的血液清除率,值为 41 mL/min/kg。 CRT0273750 (10 mg/kg;口服) 处理显示 Cmax、AUC 和 t1/2 值分别为 3.8 μM、3.2 μM.h 和 1.4 h。Animal Model:CD-1 mice
Dosage:1 mg/kg
Administration:I.v.
Result:Had a moderate blood clearance.
Animal Model:Balb-c nu/nu mice
Dosage:10, 30 and 100 mg/kg
Administration:Oral administration (Pharmacokinetic Analysis)
Result:The Cmaxs were 3.8, 10.9 and 18.1 μM, respectively.The AUCs were 3.2, 15.2 and 59.3 μM.h, respectively.The t1/2s were 1.4, 0.9 and 1.3 h, respectively.
体外研究:
CRT0273750 在生化实验和血浆胆碱释放测定实验中测得的 IC50 分别为 0.01 μM 和 0.014 μM。 CRT0273750 还可抑制 4T1 细胞的迁移,EC50 为 0.025 μM。