JHU395

Catalog No.S8892 Batch:S889201

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.)

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (11.17mM)	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 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.500mg/ml (5.59mM)	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. This compound delivers active GA to malignant peripheral nerve sheath tumour (MPNST), and significantly inhibits tumour growth without observed toxicity.

Targets

Glutamine

In vitro

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

In Vivo

In vivo, orally administered JHU395 delivers active GA to tumours with over twofold higher tumour-to-plasma exposure, and this compound significantly inhibits tumour growth in a murine flank MPNST model without observed toxicity.

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 this compound-free media; fixed concentrations of this chemical 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-Trp53^tm1Tyj Nf1^tm1Tyj/J) transgenic mice Dosages 1.2 mg/kg, 0.5 mg/kg Administration Oral gavage

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 this compound-free media; fixed concentrations of this chemical 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-Trp53^tm1Tyj Nf1^tm1Tyj/J) transgenic mice
Dosages
1.2 mg/kg, 0.5 mg/kg
Administration
Oral gavage

References

https://pubmed.ncbi.nlm.nih.gov/31594823/

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.