CRT0273750 是一种 ATX 抑制剂的先导化合物，可调节血浆中 LPA 水平，用于 ATX/LPA 依赖性癌症模型。
产品描述
CRT0273750 regulates plasma LPA levels and is suitable for in vivo studies. CRT0273750 is an autotaxin (ATX) inhibitor with IC50 of 0.014 μM.
体外活性
CRT0273750 is also shown to inhibit the migration of 4T1 cells with an EC50 of 0.025μM[1]. CRT0273750 shows high potency in both the biochemical (IC50 = 0.01 μM) and plasma choline release assay(IC50 = 0.014 μM)[1].
体内活性
CRT0273750 treatment shows the Cmax, AUC and t1/2 values of 3.8 μM, 3.2 μM.h and 1.4 h, respectively and shows a proportional increase[1].CRT0273750 has a moderate blood clearance, with value of 41 mL/min/kg[1].
Cas No.
1979939-16-6
分子式
C25H22ClF3N4O2
分子量
502.92
别名
CRT-0273750;CRT 0273750
储存和溶解度
DMSO:200 mg/ml(397.68 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
