An inhibitor of mutant IDH1 and IDH2
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Vorasidenib

Item No. 28462

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-(6-chloro-2-pyridinyl)-N2,N4-bis[(1R )-2,2,2-trifluoro-1-methylethyl]-1,3,5-triazine-2,4-diamine
CAS Number
1644545-52-7
Synonyms
  • AG-881
Molecular Formula
C14H13ClF6N6
Formula Weight
414.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.3 mg/ml
λmax
218, 284 nm
SMILES
ClC1=NC(C2=NC(N[C@H](C)C(F)(F)F)=NC(N[C@H](C)C(F)(F)F)=N2)=CC=C1
InChi Code
InChI=1S/C14H13ClF6N6/c1-6(13(16,17)18)22-11-25-10(8-4-3-5-9(15)24-8)26-12(27-11)23-7(2)14(19,20)21/h3-7H,1-2H3,(H2,22,23,25,26,27)
InChi Key
QCZAWDGAVJMPTA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

    $833

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    Product Description

    Vorsidenib is an inhibitor of mutant isocitrate dehydrogenase (IDH; IC50s = 31.9 and 31.7 nM for IDH1R132H and IDH2R140Q, respectively).1 It also inhibits wild-type-IDH1R132H and wild-type-IDH2R140Q heterodimers (IC50s = 4 and 251 nM, respectively).2 Vorsidenib decreases the production of D-2-hydroxyglutarate (2-HG; Item Nos. 25895 | 11605) in TF-1 leukemia cells expressing IDH1R132H or IDH2R140Q (IC50s = 3.2 and 14 nM, respectively). It reduces tumor growth in a TS603-IDH1R132H mouse xenograft model when administered at a dose of 50 mg/kg.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ma, R., and Yun, C.-H. Crystal structures of pan-IDH inhibitor AG-881 in complex with mutant human IDH1 and IDH2. Biochem. Biophys. Res. Commun. 503(4), 2912-2917 (2018).

    2. Yen, K., Konteatis, Z., Sui, Z., et al. AG-881, a brain penetrant, potent, pan-mutant IDH (mIDH) inhibitor for use in mIDH solid and hematologic malignancies. AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics 17(Suppl 1), (2017).

    3. Nicolay, B., Narayanaswamy, R., Amatangelo, M.D., et al. Exth-34. Combined use of pan-IDH mutant inhibitor AG-881 with radiation therapy shows added benefit in an orthotopic IDH1 mutant glioma model in vivo. Neuro. Oncol. 19(Suppl. 6), vi79 (2017).