JHU395

Catalog No.S8892

For research use only.

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

CAS No. 2079938-92-2

Purity & Quality Control

Choose Selective Glutaminase Inhibitors

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

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]

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]

Protocol (from reference)

Cell Research:

[1]

  • 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.

Animal Research:

[1]

  • 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

Molecular Weight 447.48
Formula

C22H29N3O7

Density g/mL
CAS No. 2079938-92-2
Storage 2 years -20°C liquid

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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.

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