纯度:>98% by HPLC;NMR (Conforms)
分子式:C23H19Cl2N3O4·2HCl
分子量:454.24
溶剂:DMSO (>25 mg/ml)
性状:Pale orange/yellow solid
存储:-20°C
Activity (short version):LAT1 inhibitor
Function / Pharmacology:Selective L-type amino acid transporter 1 inhibitor (LAT1 or SLC7A5; IC50 = 140 nM for 14C-leucine uptake in S2-hLAT1 cells, and 60 nM for HT29 human colon adenocarcinoma cells: growth inhibition IC50’s = 16.4 μM and 4.1 μM respectively for S2 and HT29 cells).1 Also active in HT-29 mouse xenograft models. JPH203 is active in a variety of cancer models and has progressed to clinical trials.2 It sensitized A549 and MIA Paca-2 cells to radiation by enhancing cellular senescence via mTOR downregulation3 and sensitized EGFR-expressing cancer cell lines to gefitinib therapy4. JPH203 treatment of non-small cell lung cancer cells led to downregulation of PD-L1 suggesting that LAT1 inhibition may help overcome the immune suppressive tumor microenvironment.5