JHU395 - ≥98% , CAS No.2079938-92-2

CAS: 2079938-92-2 Cat. No.: J414249 Molecular Weight: 447.48 PubChem CID: 126555751

GRADE & PURITY ≥98%

Synonyms

L-​Norleucine,6-​diazo-​N-​[[(2,​2-​dimethyl-​1-​oxopropoxy)​phenylmethoxy]​carbonyl]​-​5-​oxo-​,1-​methylethyl ester

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Overview

Information

JHU395 JHU395 is a novel orally bioavailable GA (glutamine antagonists) prodrug designed to circulate inert in plasma, but permeate and release active GA within target tissues. JHU395 delivers active GA to malignant peripheral nerve sheath tumor (MPNST), and significantly inhibits tumor growth without observed toxicity.

Targets

Glutamine

In vitro

JHU395 inhibits growth of multiple biosynthetic processes by tumors (MPNST) cells, while growth of immortalized Schwann cells is minimally affected. JHU395 induces less PARP cleavage as a marker of apoptosis in human MPNST cells. JHU395 is a plasma stable lipophilic GA prodrug which delivers DON to MPNST in an in vitro plasma to tumor cell partitioning assay measurement.

In vivo

orally administered JHU395 delivers active GA to tumors with over twofold higher tumor-to-plasma exposure, and significantly inhibits tumor growth in a murine flank MPNST model without observed toxicity.

Cell Research(from reference)

Cell lines：sNF96.2, sNF02.2, ipn02.32 

Concentrations：10 μM, 20μM 

Incubation Time：1 h, 24 h 

Specifications

Synonyms

L-​Norleucine, 6-​diazo-​N-​[[(2, ​2-​dimethyl-​1-​oxopropoxy)​phenylmethoxy]​carbonyl]​-​5-​oxo-​, 1-​methylethyl ester

Specifications & Purity

≥98%

Biochemical and Physiological Mechanisms

JHU395 is a novel orally bioavailable GA (glutamine antagonists) prodrug designed to circulate inert in plasma, but permeate and release active GA within target tissues. JHU395 delivers active GA to malignant peripheral nerve sheath tumor (MPNST), and sig

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

This product requires cold chain shipping. Ground and other economy services are not available.

Purity

≥98%

Product Properties

• ALogP: 4.148
• HBD Count: 1
• Rotatable Bond: 14

Names and Identifiers

• Canonical Smiles: CC(C)OC(=O)C(CCC(=O)C=[N+]=N)NC(=O)OC(C1=CC=CC=C1)OC(=O)C(C)(C)C
• IUPAC Name: [(5S)-5-[[2,2-dimethylpropanoyloxy(phenyl)methoxy]carbonylamino]-2,6-dioxo-6-propan-2-yloxyhexylidene]-iminoazanium
• InChIKey: KCTDLEPDMHFLHZ-KKFHFHRHSA-O
• INCHI: 1S/C22H29N3O7/c1-14(2)30-18(27)17(12-11-16(26)13-24-23)25-21(29)32-19(15-9-7-6-8-10-15)31-20(28)22(3,4)5/h6-10,13-14,17,19,23H,11-12H2,1-5H3/p+1/t17-,19?/m0/s1
• PubChem CID: 126555751
• Molecular Weight: 447.48

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro