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WZ8040

Cat. No. M1851
WZ8040 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 120 In stock
10mg USD 210 In stock
50mg USD 580 In stock
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Quality Control
Biological Activity

WZ8040 is a novel EGFR inhibitor which suppresses the growth of EGFR-T790M-containing cell lines and inhibits EGFR phosphorylation. WZ8040 has a basic chemical framework (covalent pyrimidine) which is different from that of other EGFR inhibitors. WZ8040 is 30- to 100-fold more potent against EGFR T790M, and up to 100-fold less potent against wildtype EGFR, than quinazoline-based EGFR inhibitors (HKI-272 and CL-387,785) in vitro.

Customer Product Validations & Biological Datas
Source Nature (2009). Figure 2. WZ8040
Method Immunohistochemical analysis
Cell Lines 3T3 cells
Concentrations 10 ng/ml
Incubation Time 16 h
Results These compounds were 3- to 100-fold less potent, with WZ compounds being least potent, than CL-387,785 and HKI-272 at inhibiting the growth of the EGFR WT cells.
Source Nature (2009). Figure 1. WZ8040
Method immunoblot
Cell Lines PC9 GR cells
Concentrations 10 ng/ml
Incubation Time 16 h
Results We observed a similar increased potency of the WZ compounds in the H1975 (L858R/T790M) cell line and in Ba/F3 cells harbouring EGFR T790M
Protocol
Cell Experiment
Cell lines NSCLC or Ba/F3 cells
Preparation method Cell proliferation and growth assays
NSCLC or Ba/F3 cells were exposed to treatment for 72 hours and the number of cells used per experiment determined empirically and has been previously established2,7. All experimental points were set up in six to twelve wells and all experiments were repeated at least three times. The data was graphically displayed using GraphPad Prism version 5.0 for Windows, (GraphPad Software; www.graphpad.com). The curves were fitted using a non-linear regression model with a sigmoidal dose response.
Concentrations 0~10 μM
Incubation time 72 h
Animal Experiment
Animal models EGFR-TL (T790M/L858R) mice and EGFR exon19 Deletion-T790M (TD) inducible bitransgenic mice
Formulation NMP (10% 1-methyl-2-pyrrolidinone: 90% PEG-300)
Dosages 25mg/kg daily
Administration gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 481.01
Formula C24H25ClN6OS
CAS Number 1214265-57-2
Purity 98.95%
Solubility DMSO ≥86 mg/mL
Storage at -20°C
References

Novel mutant-selective EGFR kinase inhibitors against EGFR T790M.
Zhou W, et al. Nature. 2009 Dec 24;462(7276):1070-4. PMID: 20033049.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: WZ8040 supplier, EGFR/HER2, inhibitors

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