JHU395

Catalog No.S8892 Batch:S889201

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Technical Data

Formula

C22H29N3O7
Molecular Weight 447.48 CAS No. 2079938-92-2
Solubility (25°C)* In vitro DMSO 100 mg/mL (223.47 mM)
 
 
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil
2.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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]
Density g/mL

Protocol (from reference)

Cell Assay:

[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 Study:

[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

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.