CRT0273750

• CAT Number: I025224
• CAS Number: 1979939-16-6
• Molecular Formula: C25H22ClF3N4O2
• Molecular Weight: 502.92
• Purity: ≥95%
• Synonyms: N-[(1S)-1-(4-chlorophenyl)ethyl]-3-[3-[[4-(trifluoromethoxy)phenyl]methyl]imidazo[4,5-b]pyridin-2-yl]propanamide
• InChI: InChI=1S/C25H22ClF3N4O2/c1-16(18-6-8-19(26)9-7-18)31-23(34)13-12-22-32-21-3-2-14-30-24(21)33(22)15-17-4-10-20(11-5-17)35-25(27,28)29/h2-11,14,16H,12-13,15H2,1H3,(H,31,34)/t16-/m0/s1
• InChIKey: HXYXHSDYBDFOFO-INIZCTEOSA-N
• SMILES: CC(C1=CC=C(C=C1)Cl)NC(=O)CCC2=NC3=C(N2CC4=CC=C(C=C4)OC(F)(F)F)N=CC=C3

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].

Reference

[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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