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Chemical Structure| 1037592-40-7 Chemical Structure| 1037592-40-7

Structure of JPH203
CAS No.: 1037592-40-7

Chemical Structure| 1037592-40-7

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JPH203 is a potent and selective L-type amino acid transporter 1 (LAT1) inhibitor that can be used for cancer research.

Synonyms: KYT-0353; Nanvuranlat; JPH-203SBECD

4.5 *For Research Use Only !

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Product Details of JPH203

CAS No. :1037592-40-7
Formula : C23H19Cl2N3O4
M.W : 472.32
SMILES Code : O=C(O)[C@@H](N)CC1=CC(Cl)=C(OCC2=C(OC(C3=CC=CC=C3)=N4)C4=CC(N)=C2)C(Cl)=C1
Synonyms :
KYT-0353; Nanvuranlat; JPH-203SBECD
MDL No. :MFCD30534398
InChI Key :XNRZJPQTMQZBCE-SFHVURJKSA-N
Pubchem ID :24853505

Safety of JPH203

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Xenopus oocytes 1 µM 30 minutes To evaluate the inhibitory effect of JPH203 on LAT1 Nat Commun. 2025 Feb 14;16(1):1635.
KKU-055 30 µM 15 or 30 minutes To investigate the effect of JPH203 on intracellular amino acid levels of LAT1 substrates in BTC cell lines, and found that JPH203 treatment significantly decreased the intracellular levels of LAT1 substrates. Cancer Metab. 2022 Nov 10;10(1):18.
KKU-100 30 µM 15 or 30 minutes To investigate the effect of JPH203 on intracellular amino acid levels of LAT1 substrates in BTC cell lines, and found that JPH203 treatment significantly decreased the intracellular levels of LAT1 substrates. Cancer Metab. 2022 Nov 10;10(1):18.
KKU-213 30 µM 15 or 30 minutes To investigate the effect of JPH203 on intracellular amino acid levels of LAT1 substrates in BTC cell lines, and found that JPH203 treatment significantly decreased the intracellular levels of LAT1 substrates. Cancer Metab. 2022 Nov 10;10(1):18.
MCF7 cells 0.02 –20 μg/mL 24 hours To evaluate the anticancer effect of JPH203 in combination with lapatinib, results showed that JPH203 significantly enhanced the anticancer effect of lapatinib. Bioact Mater. 2021 Jul 14;9:15-28.
T47D cells 0.02 –20 μg/mL 24 hours To evaluate the anticancer effect of JPH203 in combination with lapatinib, results showed that JPH203 significantly enhanced the anticancer effect of lapatinib. Bioact Mater. 2021 Jul 14;9:15-28.
RAW 264.7 cells 20 µM 24 hours To evaluate the effect of JPH203 on M1 macrophage polarization, results showed that JPH203 significantly downregulated the mRNA levels of pro-inflammatory factors (iNOS, TNF-α, and IL-1β) and upregulated the mRNA levels of anti-inflammatory factors (IL-10 and Arg-1) in M1 macrophages. Adv Sci (Weinh). 2024 Jun;11(22):e2400713.
Rat Cartilage Cells (RCC) 20 µM 24 hours To evaluate the protective effect of JPH203 on chondrocytes, results showed that IgG/BRJ significantly suppressed ROS production in RCC and reduced the expression of pro-inflammatory factors, enhancing the metabolic activity of chondrocytes. Adv Sci (Weinh). 2024 Jun;11(22):e2400713.
Human umbilical vein endothelial cells (HUVECs) 50 µM 24 hours JPH203 inhibited the proliferation, migration, invasion, and tube formation of HUVECs, indicating that LAT1 plays a crucial role in angiogenesis. J Exp Clin Cancer Res. 2020 Nov 30;39(1):266.
8505c 10 µM 48 hours To evaluate the effect of JPH203 on thyroid cancer cell proliferation and mTORC1 activity, results showed that JPH203 significantly reduced cell proliferation and mTORC1 signaling. J Exp Clin Cancer Res. 2018 Sep 21;37(1):234.
SW1736 10 µM 48 hours To evaluate the effect of JPH203 on thyroid cancer cell proliferation and mTORC1 activity, results showed that JPH203 significantly reduced cell proliferation and mTORC1 signaling. J Exp Clin Cancer Res. 2018 Sep 21;37(1):234.
K1 10 µM 48 hours To evaluate the effect of JPH203 on thyroid cancer cell proliferation and mTORC1 activity, results showed that JPH203 significantly reduced cell proliferation and mTORC1 signaling. J Exp Clin Cancer Res. 2018 Sep 21;37(1):234.
CCRF-CEM cells 10 µM 48 hours To evaluate the cytotoxic effect of JPH203 on CCRF-CEM cells, results showed that JPH203 significantly reduced cell viability. Cancer Metab. 2018 Mar 8;6:1.
MDA MB231 cells 10 µM 48 hours To evaluate the cytotoxic effect of JPH203 on MDA MB231 cells, results showed that JPH203 had a minor cytotoxic effect on MDA MB231 cells. Cancer Metab. 2018 Mar 8;6:1.
Pancreatic cancer MIA PaCa-2 cells 3 µM 72 hours To evaluate the inhibitory effects of JPH203 combined with cytotoxic anticancer drugs on cell growth, the results showed that JPH203 combined with all tested cytotoxic anticancer drugs significantly inhibited cell growth, especially when combined with gemcitabine. Cancer Cell Int. 2023 Jun 15;23(1):116.
Pancreatic cancer HPAC cells 6 µM 72 hours To evaluate the inhibitory effects of JPH203 combined with gemcitabine on cell growth, the results showed that the combination significantly inhibited cell growth. Cancer Cell Int. 2023 Jun 15;23(1):116.
Pancreatic cancer PANC-1 cells 30 µM 72 hours To evaluate the inhibitory effects of JPH203 combined with gemcitabine on cell growth, the results showed that the combination significantly inhibited cell growth. Cancer Cell Int. 2023 Jun 15;23(1):116.
Pancreatic cancer SUIT-2 cells 12 µM 72 hours To evaluate the inhibitory effects of JPH203 combined with gemcitabine on cell growth, the results showed that the combination significantly inhibited cell growth. Cancer Cell Int. 2023 Jun 15;23(1):116.
Biliary tract cancer HuCCT1 cells 1.3 µM 72 hours To evaluate the inhibitory effects of JPH203 combined with gemcitabine on cell growth, the results showed that the combination significantly inhibited cell growth. Cancer Cell Int. 2023 Jun 15;23(1):116.
Biliary tract cancer KKU-055 cells 0.9 µM 72 hours To evaluate the inhibitory effects of JPH203 combined with gemcitabine on cell growth, the results showed that the combination significantly inhibited cell growth. Cancer Cell Int. 2023 Jun 15;23(1):116.
Biliary tract cancer KKU-100 cells 8 µM 72 hours To evaluate the inhibitory effects of JPH203 combined with gemcitabine on cell growth, the results showed that the combination significantly inhibited cell growth. Cancer Cell Int. 2023 Jun 15;23(1):116.
Biliary tract cancer KKU-213 cells 7 µM 72 hours To evaluate the inhibitory effects of JPH203 combined with gemcitabine on cell growth, the results showed that the combination significantly inhibited cell growth. Cancer Cell Int. 2023 Jun 15;23(1):116.
LNCaP 10 µM 96 hours To evaluate the effect of JPH203 on thyroid cancer cell proliferation and mTORC1 activity, results showed that JPH203 significantly reduced cell proliferation and mTORC1 signaling. J Exp Clin Cancer Res. 2018 Sep 21;37(1):234.
THP1 40 µM 96 hours To evaluate the antileukemic effect of JPH203 on THP1 cells, the results showed that JPH203 significantly reduced the survival rate of THP1 cells. Blood Adv. 2023 Dec 26;7(24):7525-7538.
NB4 40 µM 96 hours To evaluate the antileukemic effect of JPH203 on NB4 cells, the results showed that JPH203 significantly reduced the survival rate of NB4 cells. Blood Adv. 2023 Dec 26;7(24):7525-7538.
U937 40 µM 96 hours To evaluate the antileukemic effect of JPH203 on U937 cells, the results showed that JPH203 significantly reduced the survival rate of U937 cells. Blood Adv. 2023 Dec 26;7(24):7525-7538.
K562 40 µM 96 hours To evaluate the antileukemic effect of JPH203 on K562 cells, the results showed that JPH203 significantly reduced the survival rate of K562 cells. Blood Adv. 2023 Dec 26;7(24):7525-7538.
786-O cells 100 µM JPH203 significantly reduced phospho-mTOR levels in 786-O and ACHN cells but had a marginal effect on phospho-mTOR levels in 786-O: CLDN10A and ACHN: CLDN10A cells. Cell Commun Signal. 2024 Dec 5;22(1):588.
ACHN cells 100 µM JPH203 significantly reduced phospho-mTOR levels in 786-O and ACHN cells but had a marginal effect on phospho-mTOR levels in 786-O: CLDN10A and ACHN: CLDN10A cells. Cell Commun Signal. 2024 Dec 5;22(1):588.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice MLL-AF9 mouse model 40 μM Not used Not used Blood Adv. 2023 Dec 26;7(24):7525-7538.
BALB/c mice 4T1 subcutaneous fat pad tumor model Injection 10 mg Every two days for 28 days To study the effect of JPH203 combined with anti-PD-1 antibody treatment on tumor progression and immune cell infiltration Front Immunol. 2023 Sep 4;14:1251643
Rats Anterior cruciate ligament transection (ACLT)-induced osteoarthritis model Intra-articular injection 100 μL Every 5 days for 30 days To evaluate the therapeutic effect of IgG/BRJ in the osteoarthritis model, results showed that IgG/BRJ significantly promoted cartilage repair, reduced synovial inflammation, and increased the number of M2 macrophages. Adv Sci (Weinh). 2024 Jun;11(22):e2400713.
Nude mice MCF7 tumor model Intravenous injection 2 mg/kg Every 2 days for 6 days To evaluate the in vivo anticancer effect of JPH203 in combination with lapatinib, results showed that LJ@Trp-NPs significantly inhibited tumor growth. Bioact Mater. 2021 Jul 14;9:15-28.
C57BL/6J mice Matrigel plug assay Intravenous injection 25 mg/kg/day Once daily for 14 days JPH203 significantly suppressed the growth of MIA PaCa-2 xenograft tumors and reduced intratumoral blood vessel density, indicating that inhibiting angiogenesis by targeting endothelial LAT1 can suppress tumor growth. J Exp Clin Cancer Res. 2020 Nov 30;39(1):266.
Mice BRAFV600E/PIK3CAH1047R double-mutant mouse model Intraperitoneal injection 50 mg/kg/day 5 consecutive days/week for 45 days To evaluate the effect of JPH203 on thyroid cancer tumor growth in vivo, results showed that JPH203 significantly inhibited tumor growth. J Exp Clin Cancer Res. 2018 Sep 21;37(1):234.

Protocol

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Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.12mL

0.42mL

0.21mL

10.59mL

2.12mL

1.06mL

21.17mL

4.23mL

2.12mL

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