| SKU | Size | Availability | Price | Qty |
|---|---|---|---|---|
| W408558-1ml | 1ml | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $784.90 |
EGFR/ErbB1 Selective Inhibitors | Activators
| Specifications & Purity | 10mM in DMSO |
|---|---|
| Storage Temp | Store at -80°C |
| Shipped In | Ice chest + Ice pads |
| Product Description | Information WZ8040 is a novel mutant-selective irreversibleEGFRT790Minhibitor, does not inhibit ERBB2 phosphorylation (T798I). WZ8040 is 30- to 100-fold more potent against EGFR T790M, and up to 100-fold less potent against wild-type EGFR, than quinazoline-based EGFR inhibitors such as CL-387785 and HKI-272. WZ8040 treatment potently inhibits the growth of HCC827 (EGFR Del E746_A750), PC9 (EGFR Del E746_A750), H3255 (EGFR L858R), H1975 (EGFR L858R/T790M), and PC9 GR (EGFR Del E746_A750/T790M) with IC50 of 1 nM, 6 nM, 66 nM, 9 nM, and 8 nM, respectively. WZ8040 weakly inhibits the growth of HCC827 GR (EGFR E746_A750/MET amp), H1819 (ERBB2 amp), Calu-3 (ERBB2 amp), H1781 (ERBB2 Ins G776V, C), and HN11 (EGFR & ERBB2 WT) with IC50 of >3.3 μM, 738 nM, 915 nM, 744 nM, and 1.82 μM, respectively. WZ8040 is not toxic up to 10 μM against A549 (KRAS mutant) or H3122 (EML4-ALK) cells. In vivo
cell lines： Concentrations：Dissolved in DMSO, final concentrations ~10 μM Incubation Time：72 hours Powder Purity:≥99% |
| Canonical SMILES | CN1CCN(CC1)C2=CC=C(NC3=NC=C(Cl)C(=N3)SC4=CC(=CC=C4)NC(=O)C=C)C=C2 |
|---|---|
| Molecular Weight | 481.01 |
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| Solubility | Solubility (25°C) In vitro DMSO: 51 mg/mL (196.74 mM); Water: 51 mg/mL (196.74 mM); Ethanol: Insoluble; |
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