GSK864

SKU: orb1707237

Description

GSK864 is a selective small molecule inhibitor targeting the cancer-associated IDH1 mutants R132C, R132H, and R132G. It is a valuable research tool for investigating the role of mutant IDH1 in oncology, particularly in studies of tumor metabolism, with applications in both in vitro and in vivo experimental models.

Research Area

Metabolism Research

Key Properties

• CAS Number: 1816331-66-4
• MW: 558.6
• Purity: 97.07% (May vary between batches)
• Formula: C₃₀H₃₁FN₆O₄
• SMILES: COc1c(C)cc(NC(=O)c2nn(Cc3ccc(F)cc3)c3c2CN(C[C@]3(C)C(N)=O)C(=O)c2ccc[nH]2)cc1C
• Target: Isocitrate Dehydrogenase (IDH),Dehydrogenase
• Solubility: DMSO:100 mg/mL (179.02 mM);H2O:< 1 mg/mL (Insoluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (7.16 mM)

Bioactivity

• Target IC50:
  IDH1 (R132G):16.6 nM|IDH1 (R132H):15.2 nM|2-HG:320 nM (EC50)|IDH1 (R132C):8.8 nM
• In Vivo:
  In mice with R132C or R132H IDH1 mutant transplants treated with GSK864 (IP), the number of huCD45+ CD38+ cells showed a slight increase .
• In Vitro:
  GSK864 inhibits 2-HG production in R132C IDH1 mutant HT1080 fibrosarcoma cells (EC50: 320 nM by LCMS/MS analysis) .

Storage & Handling

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

Alternative Names

IDH1 mutants R132C, IDH1 mutants R132G, IDH1 mutants R132H, IDH1, GSK864, GSK-864, GSK 864

Compound Identifiers

PubChem CID

91864701