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JHU395

JHU395
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Purity:99.75%
ee:100%
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JHU395

Catalog No. T11717Cas No. 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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Pack SizePriceAvailabilityQuantity
1 mg$80In Stock
5 mg$197In Stock
10 mg$313In Stock
25 mg$597In Stock
50 mg$852In Stock
100 mg$1,170In Stock
500 mg$2,350In Stock
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Product Introduction

Bioactivity
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]
Chemical Properties
Molecular Weight447.48
FormulaC22H29N3O7
Cas No.2079938-92-2
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 90.0 mg/mL (201.1 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.2347 mL11.1737 mL22.3474 mL111.7368 mL
5 mM0.4469 mL2.2347 mL4.4695 mL22.3474 mL
10 mM0.2235 mL1.1174 mL2.2347 mL11.1737 mL
20 mM0.1117 mL0.5587 mL1.1174 mL5.5868 mL
50 mM0.0447 mL0.2235 mL0.4469 mL2.2347 mL
100 mM0.0223 mL0.1117 mL0.2235 mL1.1174 mL

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