EZM2302 (GSK-3359088)
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 | $2000 | Check With Us |
| 500mg | $3250 | Check With Us |
| 1g | $4875 | Check With Us |
: Cat #: V20887 CAS #: 1628830-21-6 Purity ≥ 98%
Description: EZM2302 (EZM-2302; GSK-3359088; GSK3359088) is a potent, selective, and orally bioavailable arginine methyltransferase CARM1 inhibitor with potential anticancer activity.
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- Physicochemical and Storage Information
- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 585.09 |
|---|---|
| Molecular Formula | C29H37ClN6O5 |
| CAS No. | 1628830-21-6 |
| SMILES Code | O=C(N(CC1)CCC21CN(C3=NC(C4=CC(OC[C@H](O)CNC)=CC=C4Cl)=NC(C5=C(C)ON=C5C)=C3C)C2)OC |
| Synonyms | EZM-2302; GSK-3359088; EZM 2302; GSK 3359088; EZM2302; GSK3359088; |
| Protocol | In Vitro | EZM 2302 binds to CARM1 and is a selective inhibitor of CARM1 activity (IC50=6 nM) with broad selectivity against other histone methyltransferases. Treatment of MM cell lines with EZM 2302 leads to inhibition of PABP1 and SMB methylation and cell stasis with IC50 values in the nanomolar range (9, 31 nM, respectively). EZM 2302 inhibits the in vitro proliferation of multiple hematopoietic cell lines, with day 14 IC50 values of less than 100 nM in 9 of 15 cell lines. |
|---|---|---|
| In Vivo | EZM 2302 is stable in human hepatocytes (CL<3 mL/min/kg), and moderately binds to human, mouse and rat plasma proteins with a mean fraction unbound of 0.66, 0.46 and 0.74, respectively. In mouse and rat, the plasma clearance (CL) is 43 and 91 mL/min/kg, respectively. EZM 2302 shows dose-dependent exposure and tumor growth inhibition (TGI) after 21 days in the RPMI-8226 xenograft model. Tumors in all EZM 2302 dose groups measured on day 21 show significant decreases in tumor growth compared to vehicle. |
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 | 1.7091 mL | 8.5457 mL | 17.0914 mL | 34.1828 mL |
| 5mM | 0.3418 mL | 1.7091 mL | 3.4183 mL | 6.8366 mL |
| 10mM | 0.1709 mL | 0.8546 mL | 1.7091 mL | 3.4183 mL |
| 20mM | 0.0855 mL | 0.4273 mL | 0.8546 mL | 1.7091 mL |
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
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Volume
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Molecular Weight*
The dilution calculator equation
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Volume(start)
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This equation is commonly abbreviated as: C1 V1 = C2 V2
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V1
=
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C2
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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.