JPH203 (hydrochloride)

JPH203 is an inhibitor of L-type amino acid transporter 1 (LAT1, IC50 = 0.14 µM for 14C-leucine uptake in S2 cells expressing the human transporter). It is selective for LAT1 over LAT2 (IC50 = >10 µM). JPH203 inhibits 14C-leucine uptake by, and growth of, HT-29 cells (IC50s = 0.06 and 4.1 µM, respectively). It induces apoptosis and increases levels of cleaved caspase-3, caspase-7, caspase-9, and poly(ADP-ribose) polymerase (PARP) in YD-38 oral cancer cells when used at a concentration of 3 mM. JPH203 (6.3, 12.5, and 25 mg/kg) reduces tumor growth in an HT-29 mouse xenograft model.Formal Name: O-[(5-amino-2-phenyl-7-benzoxazolyl)methyl]-3,5-dichloro-L-tyrosine, dihydrochloride. CAS Number: 1597402-27-1. Synonyms: KYT-0353. Molecular Formula: C23H19Cl2N3O4 . 2HCl. Formula Weight: 545.2. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: Slightly soluble, DMSO: Slightly soluble, Ethanol: Slightly soluble. SMILES: ClC(C=C(C=C1Cl)C[C@H](N)C(O)=O)=C1OCC2=C3C(N=C(C4=CC=CC=C4)O3)=CC(N)=C2.Cl.Cl. InChi Code: InChI=1S/C23H19Cl2N3O4.2ClH/c24-16-6-12(8-18(27)23(29)30)7-17(25)21(16)31-11-14-9-15(26)10-19-20(14)32-22(28-19)13-4-2-1-3-5-13,,/h1-7,9-10,18H,8,11,26-27H2,(H,29,30),2*1H/t18-,,/m0../s1. InChi Key: MJSAOPNUSNNYQL-NTEVMMBTSA-N.