1. Metabolic Enzyme/Protease
  2. Isocitrate Dehydrogenase (IDH)

GSK864 

Cat. No.: HY-19540 Purity: 99.36%
Data Sheet SDS Handling Instructions

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.

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GSK864 Chemical Structure

GSK864 Chemical Structure

CAS No. : 1816331-66-4

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $240 In-stock
2 mg $95 In-stock
5 mg $195 In-stock
10 mg $355 In-stock
25 mg $635 In-stock
50 mg $1100 In-stock
100 mg $1950 In-stock
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Description

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.

IC50 & Target

IC50: 8.8 nM (IDH1 mutants R132C), 15.2 nM (IDH1 mutants R132H), 16.6 nM (IDH1 mutants R132G)[1]

In Vitro

GSK864 inhibits 2-HG production in R132C IDH1 mutant HT1080 fibrosarcoma cells with an EC50 of 320 nM by LCMS/MS analysis[1].

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].

References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 1.7902 mL 8.9509 mL 17.9019 mL
5 mM 0.3580 mL 1.7902 mL 3.5804 mL
10 mM 0.1790 mL 0.8951 mL 1.7902 mL
Animal Administration
[1]

Mouse: Mice receive GSK864 (213 mg/kg, 10 mL/kg) via intraperitoneal (ip) administration. IP formulation is PG:DMSO:PEG400:H2O (16.7:3.3:40:40). Serial blood samples (~0.030 mL) are collected via the femoral artery catheter at 15, 30, 45, 60, 120, 180 min following administration[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

558.6

Formula

C₃₀H₃₁FN₆O₄

CAS No.

1816331-66-4

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 100 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
GSK864
Cat. No.:
HY-19540
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