An inhibitor of mutant IDH1
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GSK864

Item No. 18762

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(S)-1-(4-fluorobenzyl)-N3-(4-methoxy-3,5-dimethylphenyl)-7-methyl-5-(1H-pyrrole-2-carbonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine-3,7-dicarboxamide
CAS Number
1816331-66-4
Molecular Formula
C30H31FN6O4
Formula Weight
558.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlEthanol: 20 mg/mlEthanol:PBS(pH 7.2) (1:1): 0.5 mg/ml
λmax
270 nm
SMILES
O=C(NC1=CC(C)=C(OC)C(C)=C1)C2=NN(CC3=CC=C(F)C=C3)C4=C2CN(C(C5=CC=CN5)=O)C[C@]4(C)C(N)=O
InChi Code
InChI=1S/C30H31FN6O4/c1-17-12-21(13-18(2)25(17)41-4)34-27(38)24-22-15-36(28(39)23-6-5-11-33-23)16-30(3,29(32)40)26(22)37(35-24)14-19-7-9-20(31)10-8-19/h5-13,33H,14-16H2,1-4H3,(H2,32,40)(H,34,38)/t30-/m0/s1
InChi Key
DUCNNEYLFOQFSW-PMERELPUSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $41

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    1 mg

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    5 mg

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    10 mg

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    Cayman Chemical
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    Product Description

    GSK864 is an allosteric inhibitor of mutant isocitrate dehydrogenase 1 (IDH1; IC50s = 9, 15, and 17 nM for IDH1 mutants R132C, R132H, and R132G, respectively).1 It is moderately selective for mutant IDH1 over wild-type IDH1 and IDH2 mutants/wild-type. GSK864 causes a dose-dependent reduction in 2-hydroxyglutarate and overcomes the block of differentiation in acute myeloid leukemia (AML) cells expressing mutant IDH1.1 It reduces the number of leukemic blasts in mice with AML xenografts.1 See the Structural Genomics Consortium (SGC) website for more information.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Okoye-Okafor, U.C., Bartholdy, B., Cartier, J., et al. New IDH1 mutant inhibitors for treatment of acute myeloid leukemia. Nat. Chem. Biol. 11, 878-892 (2015).