WZ-3146

SKU: orb1300517

Description

WZ3146 is a potent, mutant-selective irreversible inhibitor targeting EGFR(L858R) and EGFR(E746_A750) with IC50 values of 2 nM each, while sparing ERBB2 phosphorylation (T798I). It is a valuable chemical probe for studying oncogenic EGFR signaling in both cellular and animal models of non-small cell lung cancer.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1214265-56-1
• MW: 464.95
• Purity: 98.95%
• Formula: C₂₄H₂₅ClN₆O₂
• SMILES: CN1CCN(CC1)c1ccc(Nc2ncc(Cl)c(Oc3cccc(NC(=O)C=C)c3)n2)cc1
• Target: EGFR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.1 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:86 mg/mL (184.97 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  EGFR (E746_A750):2 nM|EGFR (E746_A750/T790M):14 nM|EGFR L858R/T790M:5 nM|EGFR (L858R):2 nM|EGFR:24 nM
• In Vitro:
  WZ3146 significantly suppresses the growth of EGFR mutation containing cell lines with IC50 of 3 nM in EGFR Del E746_A750 containing HCC827 cells, 15 nM in EGFR Del E746_A750 containing PC9 cells, 29 nM in EGFR L858R/T790M containing H1975 cells and 3 nM in EGFR Del E746_A750/T790M containing PC9 GR cells.
• Cell Research:
  Growth and inhibition of growth is assessed by MTS assay. NSCLC or Ba/F3 cells are exposed to treatment for 72 hours and the number of cells used per experiment is determined empirically. All experimental points are set up in six to twelve wells and all experiments are repeated at least three times. The data is graphically displayed using GraphPad Prism version 5.0 for Windows. The curves are fitted using a non-linear regression model with a sigmoidal dose response.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, EGFR, EGFR (L858R), EGFR (L858R/T790M), EGFR (E746_A750), EGFR (E746_A750/T790M), ErbB-1, Epidermal growth factor receptor, HER1, Inhibitor, WZ3146, WZ-3146, WZ 3146

Compound Identifiers

PubChem CID

44607360