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GSK321

Chemical Structure : GSK321

CAS No.: 1816331-63-1

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GSK321 (GSK-321, GSK 321)

Catalog No.: PC-70088Not For Human Use, Lab Use Only.

GSK321 is a highly potent, selective inhibitor of mutant IDH1 with IC50s of 4.6/3.8/2.9 nM for R132H/R132C/R132G respectively.

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10 mg $218 In stock
25 mg $378 In stock
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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GSK321 is a highly potent, selective inhibitor of mutant IDH1 with IC50s of 4.6/3.8/2.9 nM for R132H/R132C/R132G respectively.
GSK321 shows modest activity against WT IDH1 (IC50=46 nM) and exhibits no inhibitory activity against IDH2.
GSK321 inhibits intracellular 2-HG production in HT1080 cells (EC50= 85 nM).

Physicochemical Properties

M.Wt 501.5624
Formula C28H28FN5O3
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

10 mM in DMSO
Chemical Name/SMILES

(R)-1-(4-fluorobenzyl)-N-(3-((S)-1-hydroxyethyl)phenyl)-7-methyl-5-(1H-pyrrole-2-carbonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine-3-carboxamide

References

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

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