CRT0273750 是 ATX 抑制剂的先导化合物，并调节血浆中 LPA 水平。CRT0273750 可用于 ATX/LPA 依赖性癌症模型。
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[1].
CRT0273750 shows high potency in both the biochemical (IC50 = 0.01 μM) and plasma choline release assay(IC50 = 0.014 μM)[1].CRT0273750 is also shown to inhibit the migration of 4T1 cells with an EC50 of 0.025μM[1].
CRT0273750 (1 mg/kg; i.v.)has a moderate blood clearance, with value of 41 mL/min/kg[1].CRT0273750 (10 mg/kg; oral administration) treatment shows the Cmax, AUC and t1/2 values of 3.8 µM, 3.2 µM.h and 1.4 h, respectively[1].CRT0273750 (10, 30 and 100 mg/kg; oral administration) shows a proportional increase[1].
[1]. Shah P, et al. Discovery of potent inhibitors of the lysophospholipase autotaxin. Bioorg Med Chem Lett. 2016;26(22):5403-5410.
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