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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $107 | In Stock | |
5 mg | $263 | In Stock | |
10 mg | $413 | In Stock | |
25 mg | $668 | In Stock | |
50 mg | $993 | In Stock | |
100 mg | $1,320 | In Stock | |
1 mL x 10 mM (in DMSO) | $297 | In Stock |
Description | IPN60090 is a novel, potent, orally bioavailable, renal-type glutaminase (GLS1)-specific inhibitor with an IC50 value of 31 nM for GLS1. IPN60090 has potential anticancer and immunostimulant/immunomodulatory activity, selectively targets, binds, and inhibits human glutaminase, and can be used to study GLS1-mediated diseases. |
Targets&IC50 | GLS1:31 nM (IC50) |
In vitro | IPN60090 has an IC50 against GLS1 and an EC50 against A549 cell proliferation of <100 nM.[1] |
In vivo | IPN-60090 (100 mg/kg; oral administration; twice daily; 30 days;) causes tumor growth inhibition. IPN-60090 is robust in vivo target engagement in a dose-dependent manner. The glutamate/glutamine ratios and the free plasma concentrations of IPN-60090 at 4 hours post-dose on both day 4 and day 28 are all decreased.[2] IPN60090 (3 mg/kg; i.v.; 10 mg/kg for p.o.) has excellent pharmacokinetic properties, with CL=4.1 mL/min/kg, t1/2=1 hour, Cmax=19 μM, F%=89%.[2] |
Alias | GLS1-IN-1 |
Molecular Weight | 532.52 |
Formula | C24H27F3N8O3 |
Cas No. | 1853164-83-6 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 27.5 mg/mL (51.64 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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