Vorasidenib (AG-881) | mutant IDH1/2 inhibitor

Chemical Structure : Vorasidenib

CAS No.: 1644545-52-7

Vorasidenib (AG-881, AG 881, AG881)

Catalog No.: PC-60534Not For Human Use, Lab Use Only.

Vorasidenib (AG-881) is a potent, oral, brain-penetrant dual inhibitor of mIDH1 and mIDH2 with IC50 of 6 nM and 12 nM for IDH1-R132H and IDH2-R140Q, respectively.

Packing	Price	Stock
5 mg	$128	In stock
10 mg	$188	In stock
25 mg	$298	In stock
50 mg	$498	In stock
100 mg		Get quote

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Biological Activity

Vorasidenib (AG-881) is a potent, oral, brain-penetrant dual inhibitor of mIDH1 and mIDH2 with IC50 of 6 nM and 12 nM for IDH1-R132H and IDH2-R140Q, respectively.

Vorasidenib (AG-881) binds both IDH1-R132H and IDH2-R140Q in the same allosteric pocket at the interface of the two monomers.

Vorasidenib (AG-881) (50 mg/kg) inhibits 2-HG levels in an orthotopic grade III mIDH1 glioma model derived from the TS603 neurosphere.

Vorasidenib (AG-881) penetrates the brain of several preclinical species and inhibits 2-HG production in glioma tissue by >97% in an orthotopic glioma mouse model.

Vorasidenib (AG-881) shows for the treatment of several cancers harboring an IDH mutation.

Physicochemical Properties

M.Wt	414.74
Formula	C14H13ClF6N6
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	6-(6-chloropyridin-2-yl)-N2,N4-bis((R)-1,1,1-trifluoropropan-2-yl)-1,3,5-triazine-2,4-diamine

References

1. Konteatis Z, et al. ACS Med Chem Lett. 2020 Jan 22;11(2):101-107.
2. Mellinghoff IK, et al. N Engl J Med. 2023 Aug 17;389(7):589-601.
3. Mellinghoff IK, et al. Nat Med. 2023 Mar;29(3):615-622.

Vorasidenib (AG-881, AG 881, AG881)

Biological Activity

Physicochemical Properties

References

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