GSK864

This product is for research use only, not for human use. We do not sell to patients.

GSK864
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Size Price Stock
100mg$1650Check With Us
250mg$2650Check With Us
500mg$3975Check With Us

Cat #: V3599 CAS #: 1816331-66-4 Purity ≥ 98%

Description: GSK864 is a novel, potent and selective 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.

References: Okoye-Okafor UC, et al. New IDH1 mutant inhibitors for treatment of acute myeloid leukemia. Nat Chem Biol. 2015 Nov;11(11):878-86.

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Molecular Weight (MW)558.60
Molecular FormulaC30H31FN6O4
CAS No.1816331-66-4
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
SMILES CodeO=C(C1=NN(CC2=CC=C(F)C=C2)C3=C1CN(C(C4=CC=CN4)=O)C[C@]3(C)C(N)=O)NC5=CC(C)=C(OC)C(C)=C5
SynonymsGSK864; GSK-864; GSK 864
ProtocolIn VitroGSK864 inhibits 2-HG production in R132C IDH1 mutant HT1080 fibrosarcoma cells with an EC50 of 320 nM by LCMS/MS analysis.
In VivoFollowing 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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM1.7902 mL8.9509 mL17.9019 mL35.8038 mL
5mM0.3580 mL1.7902 mL3.5804 mL7.1608 mL
10mM0.1790 mL0.8951 mL1.7902 mL3.5804 mL
20mM0.0895 mL0.4475 mL0.8951 mL1.7902 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.