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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
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. PMC9650822
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. PMC9650822
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. PMC9650822
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. PMC8586589
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. PMC8586589
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. PMC11165524
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. PMC11165524
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. PMC7702703
Xenopus oocytes 1 μM 30 minutes To evaluate the inhibitory effect of JPH203 on LAT1 PMC11828871
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. PMC6150977
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. PMC6150977
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. PMC6150977
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. PMC5844108
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. PMC5844108
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. PMC10268460
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. PMC10268460
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. PMC10268460
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. PMC10268460
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. PMC10268460
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. PMC10268460
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. PMC10268460
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. PMC10268460
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. PMC6150977
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. PMC10761356
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. PMC10761356
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. PMC10761356
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. PMC10761356
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. PMC11619122
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. PMC11619122

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
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. PMC8586589
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. PMC11165524
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. PMC7702703
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. PMC6150977
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 PMC10507177
Mice MLL-AF9 mouse model 40 μM Not used Not used PMC10761356

Protocol

Bio Calculators
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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