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JHU395

Catalog No. T11717   CAS 2079938-92-2

JHU395 is an orally-bioavailable prodrug of a lipophilic glutamine antagonist (GA), 6-diazo-5-oxo-L-norleucine (DON). It demonstrates delivery of DON to malignant peripheral nerve sheath tumor (MPNST) both in vitro and in vivo, resulting in significant antitumor activity in MPNST. Additionally, JHU395 exhibits plasma stability.

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JHU395 Chemical Structure
JHU395, CAS 2079938-92-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 80.00
5 mg In stock $ 197.00
10 mg In stock $ 313.00
25 mg In stock $ 597.00
50 mg In stock $ 852.00
100 mg In stock $ 1,170.00
500 mg In stock $ 2,350.00
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Purity: 99.75%
ee: 100%
Purity: 99.15%
ee: 100%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description JHU395 is an orally-bioavailable prodrug of a lipophilic glutamine antagonist (GA), 6-diazo-5-oxo-L-norleucine (DON). It demonstrates delivery of DON to malignant peripheral nerve sheath tumor (MPNST) both in vitro and in vivo, resulting in significant antitumor activity in MPNST. Additionally, JHU395 exhibits plasma stability.
In vitro JHU395 (1、10、100 μmol/L) inhibits the growth of multiple biosynthetic processes by tumor (MPNST) cells, while the 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 that delivers DON to MPNST in an in vitro plasma-to-tumor cell partitioning assay measurement.[1]
In vivo JHU395 (oral gavage; 1.2 mg/kg × 5 days, 0.5 mg/kg × 9 days) 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]
Molecular Weight 447.48
Formula C22H29N3O7
CAS No. 2079938-92-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90.0 mg/mL (201.1 mM), sonification is recommended.

TargetMolReferences and Literature

1. Lemberg KM, et al. The novel glutamine antagonist prodrug JHU395 has antitumor activity in malignant peripheralnerve sheath tumor. Mol Cancer Ther. 2020;19(2):397-408. 2. Pham K, et al. Novel Glutamine Antagonist JHU395 Suppresses MYC-Driven Medulloblastoma Growth and Induces Apoptosis. J Neuropathol Exp Neurol. 2021;80(4):336-344. 3. Nedelcovych MT, et al. N-(Pivaloyloxy)alkoxy-carbonyl Prodrugs of the Glutamine Antagonist 6-Diazo-5-oxo-l-norleucine (DON) as a Potential Treatment for HIV Associated Neurocognitive Disorders. J Med Chem. 2017;60(16):7186-7198.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

JHU395 2079938-92-2 Apoptosis JHU 395 JHU-395 inhibitor inhibit

 

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