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Ivosidenib

Chemical Structure : Ivosidenib

CAS No.: 1448347-49-6

Ivosidenib (AG-120, AG120)

Catalog No.: PC-45550Not For Human Use, Lab Use Only.

Ivosidenib (AG-120) is a potent, mutant-selective inhibitor of IDH1 (isocitrate dehydrogenase type 1) with IC50 of 12 nM for mouse IDH1 R132H.

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Biological Activity

Ivosidenib (AG-120) is a potent, mutant-selective inhibitor of IDH1 (isocitrate dehydrogenase type 1) with IC50 of 12 nM for mouse IDH1 R132H.
Ivosidenib (AG-120) shows similar potency against  IDH1-R132H (IC50=12 nM); IDH1-R132C (IC50=13 nM); IDH1-R132G (IC50=8 nM); IDH1-R132L (IC50=13 nM); IDH1-R132S (IC50=12 nM), respectively.
Ivosidenib (AG-120) (50 mg/kg and 150 mg/kg, orally gavage) suppresses tumor 2-HG concentration rapidly, with maximum inhibition (92.0% and 95.2% at the 50 mg/kg and 150 mg/kg doses, respectively).
Ivosidenib (AG-120) represent a worthwhile avenue of exploration in the treatment of IDH1-mutated tumors.

Physicochemical Properties

M.Wt 582.9609
Formula C28H22ClF3N6O3
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: ≥ 39 mg/mL

Chemical Name/SMILES

Glycinamide, 1-(4-cyano-2-pyridinyl)-5-oxo-L-prolyl-2-(2-chlorophenyl)-N-(3,3-difluorocyclobutyl)-N2-(5-fluoro-3-pyridinyl)-, (2S)-

References

1. Cuyàs E, et al. Oncotarget. 2015 May 20;6(14):12279-96.

2. Cancer Discov. 2015 Jan;5(1):4.

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