Research Area
Product Type
United States ( Change Country )
WZ8040 Chemical Structure
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Biological Activity
WZ8040 is an irreversiblely EGFR T790M inhibitor (IC50<10nM).
WZ8040 is an irreversiblely inhibitor against EGFR T790M (mutation of the gatekeeper T790 residue) which is detected in 50% of clinically resistant patients to gefitinib or erlotinib. WZ8040 has a basic chemical framework (covalent pyrimidine) which is different from that of other EGFR inhibitors. [1]
This agent 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. [1]
WZ8040 has a 300-fold lower half-maximum inhibitory concentration (IC50<10nM) against the PC9GR(delE746_A750/T790M, gefitinib-resistant) cells compared with clinical-stage inhibitors such as HKI-272. [1]
Chemical Information
| Molecular Weight (WM): | 481.01 |
|---|---|
| Formula: | C24H25ClN6OS |
| CAS No.: | 1214265-57-2 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥96mg/mL |
| Water <1mg/mL | |
| Ethanol ≥3mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
Research Area
Receptor Tyrosine Kinase >> EGFR >> EGFR Inhibitors
Angiogenesis >> EGFR >> EGFR Inhibitors
JAK / STAT >> EGFR >> EGFR Inhibitors
Angiogenesis >> EGFR >> EGFR Inhibitors
JAK / STAT >> EGFR >> EGFR Inhibitors
Notes:
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After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of WZ8040 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.
After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of WZ8040 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.
Data independently produced by Dr. Zhang of Tianjin Medical University WZ8040 purchased from Selleck
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Click to enlarge
For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of WZ8040 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 mM HCl and 0.1% Nonidet-40) was added to dissolve the formazan.
For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of WZ8040 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 mM HCl and 0.1% Nonidet-40) was added to dissolve the formazan.
Data independently produced by Dr. Yong-Weon Yi from Georgetown University Medical Center---WZ8040 purchased from Selleck WZ8040 purchased from Selleck
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After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of WZ8040 for 3h,followed by 20-minute stimolation of 100ng/ml EGF. |
Data independently produced by Dr. Zhang of Tianjin Medical University
For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of WZ8040 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 mM HCl and 0.1% Nonidet-40) was added to dissolve the formazan. |
Data independently produced by Dr. Yong-Weon Yi from Georgetown University Medical Center---WZ8040 purchased from Selleck
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