[CAS NO. 1816331-66-4] GSK864
PRODUCTS SPECIFICATIONS [1816331-66-4]
DESCRIPTION [1816331-66-4]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 558.60 |
| Molecular Formula | C30H31FN6O4 |
| SMILES | FC(C=C1)=CC=C1CN2N=C(C(NC3=CC(C)=C(OC)C(C)=C3)=O)C4=C2[C@](C(N)=O)(C)CN(C(C5=CC=CN5)=O)C4 |
3 Publications Citing Use of MCE
Summary
GSK864 is an isocitrate dehydrogenase 1 ( IDH1 ) mutant inhibitor; inhibits IDH1 mutants R132C, R132H, and R132G with IC 50 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 EC 50 of 320 nM by LCMS/MS analysis [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 179.02 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent 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 |