WZ8040

SKU: orb1300516

Description

WZ8040 is a novel, irreversible EGFR inhibitor that selectively targets the T790M mutant while sparing ERBB2 phosphorylation (T798I). It is a valuable research tool for studying resistant non-small cell lung cancer in both in vitro and in vivo experimental models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1214265-57-2
• MW: 481.01
• Purity: 97.42% (May vary between batches)
• Formula: C₂₄H₂₅ClN₆OS
• SMILES: CN1CCN(CC1)c1ccc(Nc2ncc(Cl)c(Sc3cccc(NC(=O)C=C)c3)n2)cc1
• Target: EGFR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.16 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:3 mg/mL (6.24 mM);DMSO:89 mg/mL (185.03 mM)

Bioactivity

• Target IC50:
  HCC827 cells (EGFR Del E746_A750):1 nM|H1819 cells (ErbB2 amp):738 nM|EGFR/ERBB2 (wildtype):1.82 μM (in HN11 cells)|PC9 cells (EGFR Del E746_A750):6 nM|PC9 GR cells (EGFR Del E746_A750/T790M):8 nM|HCC827 GR cells (EGFR E746_A750/MET amp):>3.3 μM|H1975 cells (EGFR L858R/T790M):9 nM|H1781 cells (ErbB2 Ins G776V, C):744 nM|Calu3 (ErbB2 amp):915 nM|H3255 cells (EGFR L858R):66 nM
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• In Vitro:
  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.
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• Cell Research:
  Cells are exposed to increasing concentrations of WZ8040 for 72 hours. Growth is assessed using the MTS survival assay.(Only for Reference)

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ErbB-1, Epidermal growth factor receptor, EGFR (T790M), EGFR, Inhibitor, HER1, mutated, inhibit, NSCLC, WZ 8040, WZ8040, WZ-8040, phosphorylation

Compound Identifiers

PubChem CID

44607531