Home Proteases Glutaminase antagonist JHU395 For research use only.

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.

JHU395 Chemical Structure

JHU395 Chemical Structure

CAS: 2079938-92-2

Purity & Quality Control

Batch: S889201 DMSO] 100 mg/mL] false] ] ] false] ] ] false Purity: 99.39%
99.39

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Biological Activity

Description 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 [1]
In vitro
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.[1]
Cell Research Cell lines sNF96.2, sNF02.2, ipn02.32
Concentrations 10 μM, 20μM
Incubation Time 1 h, 24 h
Method

Dose response curves for JHU395 is measured in a 96 well plate by alamar blue fluorescence at 590 nm. 1500-2000 cells per well are plated in standard media or media containing added purine nucleotides (guanosine monophosphate,100μM). One day later media is exchanged for JHU395-free media; fixed concentrations of JHU395 are added across the plate and cells are incubated for 72 hours prior to dye addition.
In Vivo
In vivo

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.[1]
Animal Research Animal Models C57BL6/NHsd (B6) or CD-1 male mice, NPcis (B6;129S2-Trp53tm1Tyj Nf1tm1Tyj/J) transgenic mice
Dosages 1.2 mg/kg, 0.5 mg/kg
Administration Oral gavage

Chemical Information & Solubility

Molecular Weight 447.48 Formula

C22H29N3O7
CAS No. 2079938-92-2 SDF --
Density g/mL
Smiles CC(C)OC(=O)C(CCC(=O)C=[N+]=[N-])NC(=O)OC(OC(=O)C(C)(C)C)C1=CC=CC=C1
Storage (From the date of receipt) 2 years -20°C liquid

In vitro
Batch:

DMSO : 100 mg/mL ( (223.47 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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