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GSK864

Chemical Structure : GSK864

CAS No.: 1816331-66-4

GSK864 (GSK 864;GSK-864)

Catalog No.: PC-45645Not For Human Use, Lab Use Only.

GSK864 is a compound structurally related to GSK321 with improved in vivo pharmacokinetic properties, inhibits IDH1 mutants R132C, R132H, and R132G with IC50 values of 8.8, 15.2 and 16.6 nM, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GSK864 is a compound structurally related to GSK321 with improved in vivo pharmacokinetic properties, inhibits IDH1 mutants R132C, R132H, and R132G with IC50 values of 8.8, 15.2 and 16.6 nM, respectively.
GSK864 shows the similar activity (2-HG production in R132C IDH1 mutant HT1080 fibrosarcoma cells, EC50 of 320 nM).
GSK864 reduces leukemic blasts in vivo.

Physicochemical Properties

M.Wt 558.6033
Formula C30H31FN6O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 100 mg/mL

Chemical Name/SMILES

(S)-1-(4-fluorobenzyl)-N3-(4-methoxy-3,5-dimethylphenyl)-7-methyl-5-(1H-pyrrole-2-carbonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine-3,7-dicarboxamide

References

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

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