Structure of JPH203
CAS No.: 1037592-40-7
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
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
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Batch number can be found on the product's label following the word 'Batch'.
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Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
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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 |
GHS Pictogram: |
![]() |
Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
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 |
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 |
Tags: JPH203 | LAT1–4F2hc | SLC7 | L-type amino acid transporter 1 | 4F2 cell surface antigen heavy chain | CD98 | membrane transporter | 1037592-40-7
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P263 | Avoid contact during pregnancy/while nursing. |
P264 | Wash hands thoroughly after handling. |
P265 | Wash skin thouroughly after handling. |
P270 | Do not eat, drink or smoke when using this product. |
P271 | Use only outdoors or in a well-ventilated area. |
P272 | Contaminated work clothing should not be allowed out of the workplace. |
P273 | Avoid release to the environment. |
P280 | Wear protective gloves/protective clothing/eye protection/face protection. |
P281 | Use personal protective equipment as required. |
P282 | Wear cold insulating gloves/face shield/eye protection. |
P283 | Wear fire/flame resistant/retardant clothing. |
P284 | Wear respiratory protection. |
P285 | In case of inadequate ventilation wear respiratory protection. |
P231 + P232 | Handle under inert gas. Protect from moisture. |
P235 + P410 | Keep cool. Protect from sunlight. |
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Code | Phrase |
P301 | IF SWALLOWED: |
P304 | IF INHALED: |
P305 | IF IN EYES: |
P306 | IF ON CLOTHING: |
P307 | IF exposed: |
P308 | IF exposed or concerned: |
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P310 | Immediately call a POISON CENTER or doctor/physician. |
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P378 | |
P380 | Evacuate area. |
P381 | Eliminate all ignition sources if safe to do so. |
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P391 | Collect spillage. Hazardous to the aquatic environment |
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P301 + P312 | IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell. |
P301 + P330 + P331 | IF SWALLOWED: Rinse mouth. Do NOT induce vomiting. |
P302 + P334 | IF ON SKIN: Immerse in cool water/wrap in wet bandages. |
P302 + P350 | IF ON SKIN: Gently wash with plenty of soap and water. |
P303 + P361 + P353 | IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower. |
P304 + P312 | IF INHALED: Call a POISON CENTER or doctor/physician if you feel unwell. |
P304 + P340 | IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing. |
P304 + P341 | IF INHALED: If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing. |
P305 + P351 + P338 | IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. |
P306 + P360 | IF ON CLOTHING: Rinse Immediately contaminated CLOTHING and SKIN with plenty of water before removing clothes. |
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P309 + P311 | IF exposed or if you feel unwell: call a POISON CENTER or doctor/physician. |
P332 + P313 | IF SKIN irritation occurs: Get medical advice/attention. |
P333 + P313 | IF SKIN irritation or rash occurs: Get medical advice/attention. |
P335 + P334 | Brush off loose particles from skin. Immerse in cool water/wrap in wet bandages. |
P337 + P313 | IF eye irritation persists: Get medical advice/attention. |
P342 + P311 | IF experiencing respiratory symptoms: call a POISON CENTER or doctor/physician. |
P370 + P376 | In case of fire: Stop leak if safe to Do so. |
P370 + P378 | In case of fire: |
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P370 + P380 + P375 | In case of fire: Evacuate area. Fight fire remotely due to the risk of explosion. |
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P420 | Store away from other materials. |
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P410 + P403 | Protect from sunlight. Store in a well-ventilated place. |
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P411 + P235 | Keep cool. |
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P502 | Refer to manufacturer/supplier for information on recovery/recycling |
Physical hazards | |
Code | Phrase |
H200 | Unstable explosive |
H201 | Explosive; mass explosion hazard |
H202 | Explosive; severe projection hazard |
H203 | Explosive; fire, blast or projection hazard |
H204 | Fire or projection hazard |
H205 | May mass explode in fire |
H220 | Extremely flammable gas |
H221 | Flammable gas |
H222 | Extremely flammable aerosol |
H223 | Flammable aerosol |
H224 | Extremely flammable liquid and vapour |
H225 | Highly flammable liquid and vapour |
H226 | Flammable liquid and vapour |
H227 | Combustible liquid |
H228 | Flammable solid |
H229 | Pressurized container: may burst if heated |
H230 | May react explosively even in the absence of air |
H231 | May react explosively even in the absence of air at elevated pressure and/or temperature |
H240 | Heating may cause an explosion |
H241 | Heating may cause a fire or explosion |
H242 | Heating may cause a fire |
H250 | Catches fire spontaneously if exposed to air |
H251 | Self-heating; may catch fire |
H252 | Self-heating in large quantities; may catch fire |
H260 | In contact with water releases flammable gases which may ignite spontaneously |
H261 | In contact with water releases flammable gas |
H270 | May cause or intensify fire; oxidizer |
H271 | May cause fire or explosion; strong oxidizer |
H272 | May intensify fire; oxidizer |
H280 | Contains gas under pressure; may explode if heated |
H281 | Contains refrigerated gas; may cause cryogenic burns or injury |
H290 | May be corrosive to metals |
Health hazards | |
Code | Phrase |
H300 | Fatal if swallowed |
H301 | Toxic if swallowed |
H302 | Harmful if swallowed |
H303 | May be harmful if swallowed |
H304 | May be fatal if swallowed and enters airways |
H305 | May be harmful if swallowed and enters airways |
H310 | Fatal in contact with skin |
H311 | Toxic in contact with skin |
H312 | Harmful in contact with skin |
H313 | May be harmful in contact with skin |
H314 | Causes severe skin burns and eye damage |
H315 | Causes skin irritation |
H316 | Causes mild skin irritation |
H317 | May cause an allergic skin reaction |
H318 | Causes serious eye damage |
H319 | Causes serious eye irritation |
H320 | Causes eye irritation |
H330 | Fatal if inhaled |
H331 | Toxic if inhaled |
H332 | Harmful if inhaled |
H333 | May be harmful if inhaled |
H334 | May cause allergy or asthma symptoms or breathing difficulties if inhaled |
H335 | May cause respiratory irritation |
H336 | May cause drowsiness or dizziness |
H340 | May cause genetic defects |
H341 | Suspected of causing genetic defects |
H350 | May cause cancer |
H351 | Suspected of causing cancer |
H360 | May damage fertility or the unborn child |
H361 | Suspected of damaging fertility or the unborn child |
H361d | Suspected of damaging the unborn child |
H362 | May cause harm to breast-fed children |
H370 | Causes damage to organs |
H371 | May cause damage to organs |
H372 | Causes damage to organs through prolonged or repeated exposure |
H373 | May cause damage to organs through prolonged or repeated exposure |
Environmental hazards | |
Code | Phrase |
H400 | Very toxic to aquatic life |
H401 | Toxic to aquatic life |
H402 | Harmful to aquatic life |
H410 | Very toxic to aquatic life with long-lasting effects |
H411 | Toxic to aquatic life with long-lasting effects |
H412 | Harmful to aquatic life with long-lasting effects |
H413 | May cause long-lasting harmful effects to aquatic life |
H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
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