Chemical Property of EGF816
Chemical Property:
- Appearance/Colour:Solid powder
- PKA:11.38±0.43(Predicted)
- PSA：83.36000
- Density:1.28±0.1 g/cm3(Predicted)
- LogP:4.32770
- Solubility.:Soluble in DMSO
- Purity/Quality:
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99%, *data from raw suppliers
EGF816 *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
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Description
Nazartinib is an irreversible inhibitor of mutant EGF receptors (EGFRs). It is selective for EGFR mutant cell lines, including H3255 and HCC827 lung adenocarcinoma cells (IC50s = 6.11 and 1.52 nM, respectively) and resistant H1975 non-small cell lung cancer cells (NSCLC; IC50 = 4.18 nM), over cells expressing wild-type EGFRs (IC50 = 160.6 nM for HaCaT keratinocytes). Nazartinib decreases phosphorylation of EGFR in H3255, HCC827, and H1975 cells (EC50s = 5, 1, and 3 nM, respectively) and inhibits cell proliferation (EC50s = 9, 11, and 25 nM, respectively) but does not affect cell proliferation in cell lines containing wild-type EGFR. It reduces tumor growth in an HCC827 lung adenocarcinoma mouse xenograft model when administered at doses ranging from 3 to 100 mg/kg per day for 21 days.
