1037592-40-7

O-[(5-Amino-2-phenyl-7-benzoxazolyl)methyl]-3,5-dichloro-L-tyrosine is a L-type amino acid transporter 1 (LAT1) specific and potent inhibitor that suppresses proliferation in cancer cell lines.

JPH203 (KYT-0353) selectively inhibits L-type amino acid transporter LAT1-dependent L-leucine uptake and growth in HT-29 and human LAT1-expressing S2 murine renal proximal tubule cell culturesbut not human LAT2-expressing S2 cells (IC50/GI50 = 0.06/4.10.14/16.4and >10/>1000 μMrespectively). When administered via intravenous injection (6.3-25 mg/kg/d from d0 to d13)JPH203 effectively inhibits HT-29-derived tumor growth in mice in vivo.