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Vorasidenib

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.

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

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.

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