GSK2606414

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

GSK2606414
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Cat #: V0059 CAS #: 1337531-36-8 Purity ≥ 98%

Description: GSK2606414 is a novel, potent and selective inhibitor of PERK (PRKR-like endoplasmic reticulum kinase or protein kinase R (PKR)-like endoplasmic reticulum kinase) with IC50 of 0.4 nM, displaying at least 100-fold selectivity over the other EIF2AKs assayed.

References: Axten JM, et al. Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulu

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Molecular Weight (MW)451.44
Molecular FormulaC24H20F3N5O
CAS No.1337531-36-8
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 90 mg/mL (199.36 mM)r
Water: <1 mg/mL (slightly soluble or insoluble)r
Ethanol: 19 mg/mL (42.08 mM)
SMILES CodeFC(C1=CC(CC(N2CCC3=C2C=CC(C4=CN(C)C5=NC=NC(N)=C54)=C3)=O)=CC=C1)(F)F
SynonymsGSK PERK Inhibitor; GSK2606414; GSK-2606414; GSK 2606414;
ProtocolIn VitroGSK2606414 inhibits PERK activation in cells.
In VivoGSK2606414 (50 and 150 mg/kg, p.o.) inhibits the growth of a human tumor xenograft in mice.
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
1mM2.2151 mL11.0757 mL22.1513 mL44.3027 mL
5mM0.4430 mL2.2151 mL4.4303 mL8.8605 mL
10mM0.2215 mL1.1076 mL2.2151 mL4.4303 mL
20mM0.1108 mL0.5538 mL1.1076 mL2.2151 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.