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JPH203 | LAT1 inhibitor

CAS:
1597402-27-1
Catalog Number:
10-4464
Activity:
LAT1 inhibitor
Chemical Names:
(2S)-2-Amino-3-[4-[(5-amino-2-phenyl-1,3-benzoxazol-7-yl)methoxy]-3,5-dichlorophenyl]propanoic acid dihydrochloride
Alternate Name:
KYT-0353; Nanvuralant
Molecular Weight:
545.24
Molecular Formula:
C23H19Cl2N3O4·2HCl
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
Pale orange/yellow solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

JPH203 (1597402-27-1) is a 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

References/Citations:

  1. Oda et al. (2010) L-type amino acid transporter 1 inhibitors inhibit tumor cell growth; Cancer Sci. 101 173
  2. Kanai (2022) Amino acid transporter LAT1 (SLC7A5) as a molecular target for cancer diagnosis and therapeutics; Pharmacol. Ther. 230 107964
  3. Bo et al. (2021) LAT1 inhibitor JPH203 sensitizes cancer cells to radiation by enhancing radiation-induced cellular senescence; Transl. Oncol. 14 101212
  4. Saito et al. (2018), Amino acid starvation culture condition sensitizes EGFR-expressing cancer cell lines to gefitinib-mediated cytotoxicity by inducing atypical necroptosis; Int. J. Oncol. 52 1165
  5. Liu et al. (2021), L-Type Amino Acid Transporter 1 Regulates Cancer Stemness and the Expression of Programmed Cell Death 1 Ligand 1 in Lung Cancer Cells; Int. J. Mol. Sci. 22 10955
JPH203 | LAT1 inhibitor is also available in the Cellular Metabolism Library.
CAS:
1597402-27-1
Catalog Number:
10-4464
Activity:
LAT1 inhibitor
Chemical Names:
(2S)-2-Amino-3-[4-[(5-amino-2-phenyl-1,3-benzoxazol-7-yl)methoxy]-3,5-dichlorophenyl]propanoic acid dihydrochloride
Alternate Name:
KYT-0353; Nanvuralant
Molecular Weight:
545.24
Molecular Formula:
C23H19Cl2N3O4·2HCl
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
Pale orange/yellow solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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