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GSK864

GSK864 Structure
GSK864
GSK864 Property
  • Boiling point 782.9±60.0 °C(Predicted)
  • Density 1.37±0.1 g/cm3(Predicted)
  • storage temp. 2-8°C
  • solubility DMF:20.0(Max Conc. mg/mL);35.8(Max Conc. mM)
    DMSO:60.0(Max Conc. mg/mL);107.41(Max Conc. mM)
    Ethanol:20.0(Max Conc. mg/mL);35.8(Max Conc. mM)
    Ethanol:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);0.9(Max Conc. mM)
  • pka 11.73±0.70(Predicted)
  • form powder
  • color white to beige
  • optical activity [α]/D -66 to -76°, c = 0.5 in methanol
  • UNSPSC Code 12352200
  • NACRES NA.77
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal word
  • Hazard statements
  • Precautionary statements
GSK864 Price More Price(2)
  • Brand: Sigma-Aldrich(India)
  • Product number: SML1757
  • Product name : GSK864
  • Purity: ≥98% (HPLC)
  • Packaging: 5MG
  • Price: ₹32085.3
  • Updated: 2022/06/14
  • Buy: Buy
  • Brand: Sigma-Aldrich(India)
  • Product number: SML1757
  • Product name : GSK864
  • Purity: ≥98% (HPLC)
  • Packaging: 25MG
  • Price: ₹125570
  • Updated: 2022/06/14
  • Buy: Buy

GSK864 Chemical Properties,Usage,Production

  • Uses GSK864 is an isocitrate dehydrogenase 1 (IDH1) mutant inhibitor; inhibits IDH1 mutants R132C, R132H, and R132G with IC50 values of 8.8, 15.2 and 16.6 nM.
  • Biochem/physiol Actions GSK864 is a cell penetrant, potent and selective allosteric inhibitor of isocitrate dehydrogenase 1 (IDH1) that potently inhibits intracellular 2-hydroxyglutarate (2-HG) production in HT-1080 cells. It appears that GSK864 binds to an allosteric binding site and locks WT and mutant IDH1s in a catalytically inactive conformation. GSK864 is a highly bioavailable analog of GSK321. For full characterization details, please visit the GSK864 probe summary on the Structural Genomics Consortium (SGC) website.To learn about other SGC chemical probes for protein targets, visit sigma.com/sgc
  • in vivo

    Following intraperitoneal (IP) administration in CD-1 mice, significant concentrations of GSK864 are maintained in peripheral blood samples of mice for up to 24 hours. Analysis of BM cells for expression of markers of early differentiation reveals slightly increased numbers of huCD45+CD38+ cells in R132C or R132H IDH1 mutant engrafted mice treated with GSK864[1].

  • IC 50 IDH1
  • References [1] Okoye-Okafor UC, et al. New IDH1 mutant inhibitors for treatment of acute myeloid leukemia. Nat Chem Biol. 2015 Nov;11(11):878-86. DOI:10.1038/nchembio.1930
GSK864 Preparation Products And Raw materials
Raw materials
Preparation Products
GSK864 Suppliers
Global(65)Suppliers
  • Supplier：
    TargetMol Chemicals Inc.
  • Tel：+1-781-999-5354<br/>+1-00000000000
  • Email：marketing@targetmol.com
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    InvivoChem
  • Tel：+1-708-310-1919<br/>+1-13798911105
  • Email：sales@invivochem.cn
  • Country：United States
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  • Supplier：
    Aladdin Scientific
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  • Email：tp@aladdinsci.com
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  • Supplier： MedChemexpress LLC
  • Tel：021-58955995
  • Email：sales@medchemexpress.cn
  • Country：United States
  • ProdList：4861
  • Advantage：58
GSK864 Spectrum
1816331-66-4, GSK864Related Search:
  • 抑制剂
  • 细胞生物学试剂
  • C30H31FN6O4
  • 异柠檬酸脱氢酶1(IDH1)突变体抑制剂(GSK864)
  • (S)-1-(4-氟苄基)-N3-(4-甲氧基-3,5-二甲基苯基)-7-甲基-5-(1H-吡咯-2-羰基)-4,5,6,7-四氢-1H-吡唑并[4,3-C]吡啶-3,7-二甲酰胺
  • 化合物 GSK864
  • 化合物 T15442
  • 1816331-66-4
  • (7S)-1-[(4-fluorophenyl)methyl]-N3-(4-methoxy-3,5-dimethylphenyl)-7-methyl-5-(1H-pyrrole-2-carbonyl)-1H,4H,5H,6H,7H-pyrazolo[4,3-c]pyridine-3,7-dicarboxamide
  • GSK864,GSK-864
  • GSK864 >=98% (HPLC)
  • 1H-Pyrazolo[4,3-c]pyridine-3,7-dicarboxamide, 1-[(4-fluorophenyl)methyl]-4,5,6,7-tetrahydro-N3-(4-methoxy-3,5-dimethylphenyl)-7-methyl-5-(1H-pyrrol-2-ylcarbonyl)-, (7S)-
  • GSK864

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