GSK343
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 | $710 | Check With Us |
| 500mg | $1250 | Check With Us |
| 1g | $1875 | Check With Us |
: Cat #: V0380 CAS #: 1346704-33-3 Purity ≥ 98%
Description: GSK343 is a novel, highly potent and selective inhibitor of H3-lysine 27 (H3K27) methyltransferase EZH2 with antineoplastic activity.
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- Physicochemical and Storage Information
- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 541.69 |
|---|---|
| Molecular Formula | C31H39N7O2 |
| CAS No. | 1346704-33-3 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 10 mg/mL (18.5 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: 4 mg/mL (7.4 mM) | |
| SMILES Code | O=C(C1=CC(C2=CC(N3CCN(C)CC3)=NC=C2)=CC4=C1C=NN4C(C)C)NCC5=C(CCC)C=C(C)NC5=O |
| Synonyms | GSK-343; GSK 343; GSK343 |
| Protocol | In Vitro | GSK343, which contains an n-propyl group at the 4-position of the pyridone, has EZH2 Kiapp=1.2±0.2 nM. In this 6-day proliferation assay, among the cell lines evaluated in this study, the prostate cancer cell line LNCaP is the most sensitive to EZH2 inhibition, with growth IC50 value of 2.9 μM for GSK343. |
|---|---|---|
| In Vivo | Compare with the controls, GSK343 (5 mg/kg)-treated mice exhibits significantly inhibited tumor growth. The average tumor volume and weight of the GSK343-treated cohort is remarkably reduced. As early as 20 days post-implantation, a significant reduction in tumor growth is observed in the GSK343-treated cohort relative to the control cohort; this difference persisted through the remainder of the study. In addition, compare with the control cohort, the GSK343-treated animals in the xenograft model show a remarkable increase in messenger RNA levels of E-cadherin but a significant decrease in vimentin messenger RNA levels. |
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 | 1.8461 mL | 9.2304 mL | 18.4607 mL | 36.9215 mL |
| 5mM | 0.3692 mL | 1.8461 mL | 3.6921 mL | 7.3843 mL |
| 10mM | 0.1846 mL | 0.9230 mL | 1.8461 mL | 3.6921 mL |
| 20mM | 0.0923 mL | 0.4615 mL | 0.9230 mL | 1.8461 mL |
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
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Volume
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Molecular Weight*
The dilution calculator equation
Concentration(start)
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Volume(start)
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This equation is commonly abbreviated as: C1 V1 = C2 V2
Concentration(start)
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V1
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C2
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Volume(final)
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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.