WZ4002
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 |
---|---|---|
500mg | $450 | Check With Us |
1g | $750 | Check With Us |
5g | $1900 | Check With Us |
Cat #: V0552 CAS #: 1213269-23-8 Purity ≥ 98%
Description: WZ4002 (WZ-4002) is a covalent/irreversible and mutant-selective EGFR (e.g. L858R/T790M) 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) | 494.18 |
---|---|
Molecular Formula | C25H27ClN6O3 |
CAS No. | 1213269-23-8 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: 13 mg/mL (26.3 mM)r |
Water: <1 mg/mLr | |
Ethanol: <1 mg/mL | |
Solubility In Vivo | 30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL |
SMILES Code | C=CC(NC1=CC=CC(OC2=NC(NC3=CC=C(N4CCN(C)CC4)C=C3OC)=NC=C2Cl)=C1)=O |
Synonyms | WZ-4002; WZ 4002; WZ4002; |
Protocol | In Vitro | WZ4002 increases cellular potency correlated with inhibition of EGFR, AKT and ERK1/2 phosphorylation in NSCLC cell lines and EGFR phosphorylation in NIH-3T3 cells expressing different EGFRT790M mutant alleles. WZ4002 inhibits EGFR kinase activity of recombinant L858R/T790M protein more potently than of WT EGFR. |
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In Vivo | In a pharmacodynamic study WZ4002 effectively inhibits EGFR, AKT and ERK1/2 phosphorylation which is associated with a significant increase in TUNEL positive and a significant decrease in Ki67 positive cells compared to vehicle alone treated mice. In a 2 week efficacy study, WZ4002 treatment results in significant tumor regressions compared to vehicle alone in both T790M containing murine models. Histological evaluation of the lungs following treatment confirms significant resolution of the tumor nodules with only few small residual nodules and nodule remnants that has evidence of treatment effect with decreased cellularity and increased fibrosis consistent with remodeling/scarring. |
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 | 2.0236 mL | 10.1178 mL | 20.2355 mL | 40.4711 mL |
5mM | 0.4047 mL | 2.0236 mL | 4.0471 mL | 8.0942 mL |
10mM | 0.2024 mL | 1.0118 mL | 2.0236 mL | 4.0471 mL |
20mM | 0.1012 mL | 0.5059 mL | 1.0118 mL | 2.0236 mL |
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Step One: Enter information below
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Step Two: Enter the in vivo formulation
%DMSO
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%ddH2O
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Method for preparing DMSO master liquid:
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,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.