CRT0273750

CRT0273750 is an autotaxin (ATX) inhibitor and modulates LPA levels in plasm (IC 50 = 0.014 μM). CRT0273750 can be used in ATX/LPA-dependent models of cancer In Vitro CRT0273750 shows high potency in both the biochemical (IC 50 = 0.01 μM) and plasma choline release assay(IC 50 = 0.014 μM). CRT0273750 is also shown to inhibit the migration of 4T1 cells with an EC50 of 0.025μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo CRT0273750 (1 mg/kg; i.v.)has a moderate blood clearance, with value of 41 mL/min/kg . CRT0273750 (10 mg/kg; oral administration) treatment shows the C max , AUC and t 1/2 values of 3.8 µM, 3.2 µM.h and 1.4 h, respectively . CRT0273750 (10, 30 and 100 mg/kg; oral administration) shows a proportional increase . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 C max s were 3.8, 10.9 and 18.1 µM, respectively. The AUCs were 3.2, 15.2 and 59.3 µM.h, respectively. The t 1/2 s were 1.4, 0.9 and 1.3 h, respectively. Form:Solid IC50& Target:IC50: 0.014 μM (plasma CRA)

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