NANVURANLAT

Investigational

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=C3OC(=NC3=CC(N)=C2)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

HIDE SMILES / InChI

Molecular Formula	C23H19Cl2N3O4
Molecular Weight	472.321
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Approval Year

Targets

Targets

Primary Target	Pharmacology	Condition	Potency
Large neutral amino acids transporter small subunit 1 3	Inhibitor 8,297

Substance Class	Chemical
Record UNII	CEDO9QXYZK
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

NANVURANLAT

Official Name

English

KYT-0353

Code

English

JPH 203

Code

English

L-TYROSINE, O-((5-AMINO-2-PHENYL-7-BENZOXAZOLYL)METHYL)-3,5-DICHLORO-

Systematic Name

English

nanvuranlat [INN]

Common Name

English

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Classification Tree

Code System

Code

Designated

FDA ORPHAN DRUG

872522

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Code System

Code

Type

Description

MANUFACTURER PRODUCT INFORMATION

JPH-203

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).

SMS_ID

300000032239

PRIMARY

PUBCHEM

24853505

PRIMARY

NCI_THESAURUS

C179105

PRIMARY

FDA UNII

CEDO9QXYZK

PRIMARY

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Related Record

Type

Details


					4KHYO80GXC

CD98

TARGET -> INHIBITOR

Interaction Type:

INHIBITOR

Qualification:

IC50

Amount:

140 NANOMOLAR (average)
IN LAT1 S2 CELLS


					ZJK9MX8G8Q

NANVURANLAT DIHYDROCHLORIDE

SALT/SOLVATE -> PARENT

Amount:

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Related Record

Type

Details


					TK2NS5G8OB

N-ACETYL JPH-203

IMPURITY -> PARENT

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Type

Details


					CEDO9QXYZK

NANVURANLAT

ACTIVE MOIETY

Comments:

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.


					CEDO9QXYZK

NANVURANLAT

ACTIVE MOIETY

Comments:

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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