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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $80 | In Stock | |
5 mg | $197 | In Stock | |
10 mg | $313 | In Stock | |
25 mg | $597 | In Stock | |
50 mg | $852 | In Stock | |
100 mg | $1,170 | In Stock | |
500 mg | $2,350 | In Stock |
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), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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