GSK461364

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

GSK461364
For small sizes, please check our retail website as below: www.invivochem.com
Size Price Stock
250mg$1050Check With Us
500mg$1650Check With Us
1g$2475Check With Us

Cat #: V1576 CAS #: 929095-18-1 Purity ≥ 98%

Description: GSK-461364 (GSK461364; GSK 461364) is a novel, potent, selective, reversible and ATP-competitive small molecule Polo-like kinase 1 (PLK1) inhibitor with potential antitumor activity.

References: Olmos D, et al. Phase I study of GSK461364, a specific and competitive Polo-like kinase 1 inhibitor, in patients with advanced solid malignancies. Clin Cancer Res. 2011 May 15;17(10):3420-30.

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Molecular Weight (MW)543.6
Molecular FormulaC27H28F3N5O2S
CAS No.929095-18-1
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 10 mg/mL (18.4 mM)r
Water:<1 mg/mLr
Ethanol: 30 mg/mL (55.2 mM)
Solubility In Vivo1% DMSO+30% polyethylene glycol+1% Tween 80: 30 mg/mL
SynonymsGSK461364; GSK 461364; GSK-461364; GSK461364A; GSK 461364A; GSK-461364A; (R)-5-(6-((4-methylpiperazin-1-yl)methyl)-1H-benzo[d]imidazol-1-yl)-3-(1-(2-(trifluoromethyl)phenyl)ethoxy)thiophene-2-carboxamide
ProtocolIn VitroGSK461364 is a potent, selective, and reversible ATP-competitive Plk1 inhibitor (Ki, 2.2 nM) with at least 390-fold greater selectivity for Plk1 than for Plk2 and Plk3 and 1,000-fold greater selectivity than for a panel of 48 other kinases
In VivoGSK461364 (50 mg/kg) exhibits various degrees of tumor growth delay (TGD) in multiple xenograft tumor models by i.p. one dose every 2 days repeated twelve times (q2d×12)
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
1mM1.8396 mL9.1979 mL18.3959 mL36.7918 mL
5mM0.3679 mL1.8396 mL3.6792 mL7.3584 mL
10mM0.1840 mL0.9198 mL1.8396 mL3.6792 mL
20mM0.0920 mL0.4599 mL0.9198 mL1.8396 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.