CAS No. 1816331-66-4

Batch: Purity:99.01
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GSK864 Chemical Structure
Chemical Structure
Check the GSK864 product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Chemical Information

IUPAC Name (7S)-1-[(4-fluorophenyl)methyl]-3-N-(4-methoxy-3,5-dimethylphenyl)-7-methyl-5-(1H-pyrrole-2-carbonyl)-4,6-dihydropyrazolo[4,5-c]pyridine-3,7-dicarboxamide
CAS Number 1816331-66-4
Molecular Formula

C30H31FN6O4
Molecular Weight (MW) 558.60
InChIKey DUCNNEYLFOQFSW-PMERELPUSA-N

Biological Activity

GSK864 is a potent, cell-penetrant, and selective inhibitor of mutant isocitrate dehydrogenase 1 (IDH1), specifically targeting the IDH1-R132H, IDH1-R132C, and IDH1-R132G variants. By selectively inhibiting mutant IDH1 enzymatic activity, GSK864 suppresses the production of the oncometabolite 2-hydroxyglutarate (2-HG) and blocks downstream oncogenic signaling, leading to cellular differentiation and impaired cell proliferation in acute myeloid leukemia and other mutant IDH1-driven malignancy models. [1]

How to Prepare Stock Solution?

Concentration Volume Mass
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Solubility

Batch:
All in vitro solubility values are batch-tested experimental data (non-literature values).
Solvent Solubility & Note
DMSO 100 mg/mL (179.01 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO. The recommended stock concentration is 10 mM in DMSO.)
Water Insoluble
Ethanol Insoluble
FAQ
Q: Why does a DMSO stock precipitate in media/saline?
A: It is caused by unheated aqueous media (supersaturation), local solvent shock, or incorrect mixing sequence.
How to fix it?
  • Preheat media/saline to 37°C.
  • Mix rapidly (pipette/vortex) upon addition.
  • For complex mixes, always add the aqueous phase last.
  • Re-dissolve minor precipitates with a 37°C water bath and sonication (≤30 min).

Reference

[1] Okoye-Okafor UC, et al. Nat Chem Biol. 2015;11(11):878-86.

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Note: Technical data last updated: Sep 1, 2026.