A potent, selective inhibitor of mutant IDH2
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AGI-6780

Item No. 14639

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-cyclopropyl-4-(3-thienyl)-3-[[[[3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-benzenesulfonamide
CAS Number
1432660-47-3
Molecular Formula
C21H18F3N3O3S2
Formula Weight
481.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS(pH 7.2) (1:4): 0.2 mg/mlEthanol: 5 mg/ml
λmax
245 nm
SMILES
O=S(C1=CC(NC(NC2=CC=CC(C(F)(F)F)=C2)=O)=C(C3=CSC=C3)C=C1)(NC4CC4)=O
InChi Code
InChI=1S/C21H18F3N3O3S2/c22-21(23,24)14-2-1-3-16(10-14)25-20(28)26-19-11-17(32(29,30)27-15-4-5-15)6-7-18(19)13-8-9-31-12-13/h1-3,6-12,15,27H,4-5H2,(H2,25,26,28)
InChi Key
CCAWRGNYALGPQH-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

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    Cayman Chemical
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    Product Description

    AGI-6780 is a potent, selective inhibitor of mutant IDH2 with an IC50 value of 23 nM.1 It binds allosterically at the dimer interface of mutant IDH2-R140Q, inhibiting 2-HG formation in human glioblastoma U87 and TF-1 cells expressing IDH2-R140Q with IC50 values of 11 and 18 nM, respectively.1 In primary human acute myelogenous leukemia cells, AGI-6780 suppressed cell growth and induced differentiation of immature blast cells toward macrophage and granulocytic lineages.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wang, F., Travins, J., DeLaBarre, B., et al. Targeted inhibition of mutant IDH2 in leukemia cells induces cellular differentiation. Science 340(6132), 622-626 (2013).

    2. Lidington, E.A., Steinberg, R., Kinderlerer, A.R., et al. A role for proteinase-activated receptor 2 and PKC-ε in thrombin-mediated induction of decay-accelerating factor on human endothelial cells. Am. J. Physiol. Cell Physiol. 289(6), 1437-1447 (2005).