IPN60090

SKU: orb1709597

Description

IPN60090 is a potent and orally bioavailable specific inhibitor of renal-type glutaminase (GLS1) with an IC50 of 31 nM. It is a research tool for studying cancer metabolism and immunomodulation, with applications in both in vitro enzymatic assays and in vivo preclinical models of GLS1-mediated diseases.

Research Area

Metabolism Research, Protein Biochemistry

Key Properties

• CAS Number: 1853164-83-6
• MW: 532.52
• Purity: >99.99% (May vary between batches)
• Formula: C₂₄H₂₇F₃N₈O₃
• SMILES: CNC(=O)c1cn(C[C@H](F)CCc2ccc(NC(=O)Cc3cc(OC4CC(F)(F)C4)cc(C)n3)nn2)nn1
• Target: transporter,Glutaminase
• Solubility: DMSO:27.5 mg/mL (51.64 mM);10% DMSO+90% Corn Oil:2 mg/mL (3.76 mM)

Bioactivity

• Target IC50:
  GLS1:31 nM (IC50)
• 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. 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%.
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• In Vitro:
  IPN60090 has an IC50 against GLS1 and an EC50 against A549 cell proliferation of <100 nM.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Glutaminase GLS1 (KGA), GLS1, GLS1-IN-1, IPN60090, IPN-60090, IPN 60090

Compound Identifiers

PubChem CID

118627280