Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C23H19Cl2N3O4 |
| Molecular Weight | 472.321 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
N[C@@H](CC1=CC(Cl)=C(OCC2=CC(N)=CC3=C2OC(=N3)C4=CC=CC=C4)C(Cl)=C1)C(O)=O
InChI
InChIKey=XNRZJPQTMQZBCE-SFHVURJKSA-N
InChI=1S/C23H19Cl2N3O4/c24-16-6-12(8-18(27)23(29)30)7-17(25)21(16)31-11-14-9-15(26)10-19-20(14)32-22(28-19)13-4-2-1-3-5-13/h1-7,9-10,18H,8,11,26-27H2,(H,29,30)/t18-/m0/s1
| Molecular Formula | C23H19Cl2N3O4 |
| Molecular Weight | 472.321 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Approval Year
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
463.1 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32198649/ |
12 mg/m² single, intravenous dose: 12 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
JPH-203 plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
887.8 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32198649/ |
25 mg/m² single, intravenous dose: 25 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
JPH-203 plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
1460.5 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32198649/ |
40 mg/m² single, intravenous dose: 40 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
JPH-203 plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
2094.3 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32198649/ |
60 mg/m² single, intravenous dose: 60 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
JPH-203 plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
3022.5 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32198649/ |
85 mg/m² single, intravenous dose: 85 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
JPH-203 plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
| Substance Class |
Chemical
Created
by
admin
on
Edited
Tue Apr 01 17:48:50 GMT 2025
by
admin
on
Tue Apr 01 17:48:50 GMT 2025
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| Record UNII |
CEDO9QXYZK
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| Record Status |
Validated (UNII)
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| Record Version |
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Official Name | English | ||
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Preferred Name | English | ||
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FDA ORPHAN DRUG |
872522
Created by
admin on Tue Apr 01 17:48:50 GMT 2025 , Edited by admin on Tue Apr 01 17:48:50 GMT 2025
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| Code System | Code | Type | Description | ||
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JPH-203
Created by
admin on Tue Apr 01 17:48:50 GMT 2025 , Edited by admin on Tue Apr 01 17:48:50 GMT 2025
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PRIMARY | MedKoo CAT#: 406760; CAS#: 1037592-40-7;Description: JPH203, also known as KYT-0353, is a potent and selective LAT1 selective ( L-type amino acid transporter 1) inhibitor. JPH203 can very potently inhibit l-leucine uptake. JPH203 inhibits YD-38 cell growth. JPH203 up-regulated the population of apoptotic YD-38 cells through the activation of apoptotic factors, including caspases and PARP. (last updated: 7/13/2016). | ||
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300000032239
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24853505
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C179105
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CEDO9QXYZK
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1037592-40-7
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11602
Created by
admin on Tue Apr 01 17:48:50 GMT 2025 , Edited by admin on Tue Apr 01 17:48:50 GMT 2025
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PRIMARY | INN |
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TARGET -> INHIBITOR |
INHIBITOR
IC50
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SALT/SOLVATE -> PARENT |
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IMPURITY -> PARENT |
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ACTIVE MOIETY |
The present studies illustrate that KYT-0353 inhibited (14)C-leucine uptake and cell growth in human colon cancer-derived HT-29 cells; IC(50)s were 0.06 microm and 4.1 microm, respectively. KYT-0353 also inhibited (14)C-leucine uptake in mouse renal proximal tubule cells expressing l-type amino acid transporter 1, and inhibited cell growth; IC(50)s were 0.14 microm and 16.4 microm, respectively. Compared to control animals, intravenously administered KYT-0353 (12.5 mg/kg and 25.0 mg/kg) showed statistically significant growth inhibition against HT-29 tumors transplanted to nude mice with maximal inhibition ratios of 65.9% and 77.2%, respectively. Body weight increase with time--a safety indicator--was slightly depressed at 12.5 mg/kg and 25.0 mg/kg with maximal ratios of 3.7% (day 2) and 6.3% (day 11), respectively. Thus, KYT-0353 showed significant growth inhibitory effects on HT-29 cells both in vitro and in vivo, whereas it only caused a slight body weight depression. Therefore, KYT-0353 appears to have potential as a novel anti-tumor agent, presumably via selective in vivol-type amino acid transporter 1 inhibition.
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ACTIVE MOIETY |
Originator: J-Pharma; Class: Antineoplastic; Mechanism of Action: Amino acid transport system L inhibitor; Orphan Drug Status: No; On Fast track: No; New Molecular Entity: Yes; Highest Development Phase: Phase I for Solid tumours; Most Recent Events: 19 Feb 2015 JPH 203 has patent protection in Japan, 19 Jan 2015 Phase-I clinical trials in Solid tumours (Metastatic disease) in Japan (IV) (UMIN000016546)
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