GSK503
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $810 | Check With Us |
| 500mg | $1350 | Check With Us |
| 1g | $2025 | Check With Us |
: Cat #: V0387 CAS #: 1346572-63-1 Purity ≥ 98%
Description: GSK503 (GSK-503) is a novel, potent and specific inhibitor of Enhancer of zeste homolog 2 (EZH2) methyltransferase inhibitor with potential antitumor activity.
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- Physicochemical and Storage Information
- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 526.67 |
|---|---|
| Molecular Formula | C31H38N6O2 |
| CAS No. | 1346572-63-1 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 100 mg/mL (189.8 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: 26 mg/mL warmed (49.4 mM) | |
| SMILES Code | O=C(C1=CC(C2=CC=C(N3CCN(C)CC3)N=C2)=CC4=C1C(C)=CN4C(C)C)NCC5=C(C)C=C(C)NC5=O |
| Synonyms | GSK 503; GSK503; GSK-503 |
| Protocol | In Vitro | GSK503 inhibits the methyltransferase activity of wild type and mutant EZH2 with similar potency (Kiapp=3-27 nM) and is structurally related to GSK126 and GSK343. GSK503 is >200 fold selective over EZH1 (Kiapp=636 nM) and >4000 fold selective over other histone methyltransferases. |
|---|---|---|
| In Vivo | In a melanoma mouse model, conditional EZH2 ablation as much as treatment with the GSK503 stabilizes the disease through inhibition of growth and virtually abolishes metastases formation without affecting normal melanocyte biology[2]. GSK503 displays favorable pharmacokinetics in mice. GSK503, but not vehicle, prevents the formation of germinal center after SRBC or NP-KLH immunization, phenocopying the Ezh2 null phenotype. GSK503 treatment leads to reduced numbers of GC B-cells by flow cytometry, reduces number and volume of GCs by immunohistochemistry, and impairs formation high affinity antibodies. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 1.8987 mL | 9.4936 mL | 18.9872 mL | 37.9744 mL |
| 5mM | 0.3797 mL | 1.8987 mL | 3.7974 mL | 7.5949 mL |
| 10mM | 0.1899 mL | 0.9494 mL | 1.8987 mL | 3.7974 mL |
| 20mM | 0.0949 mL | 0.4747 mL | 0.9494 mL | 1.8987 mL |
The molarity calculator equation
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The dilution calculator equation
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This equation is commonly abbreviated as: C1 V1 = C2 V2
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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.