Nazartinib (EGF816, NVS-816) is a covalent, irreversible, mutant-selective EGFR inhibitor that has nanomolar inhibitory potency against activating mt (L858R, ex19del) and T790M mt, with up to 60-fold selectivity over wild type (wt) EGFR in vitro.
| Pack Size | Availability | Price/USD | Quantity |
|---|---|---|---|
| 1 mg | In stock | $ 102 | |
| 2 mg | In stock | $ 183 | |
| 4 mg | In stock | $ 308 | |
| 10 mg | In stock | $ 518 | |
| 20 mg | In stock | $ 828 |
| Description | Nazartinib (EGF816, NVS-816) is a covalent, irreversible, mutant-selective EGFR inhibitor that has nanomolar inhibitory potency against activating mt (L858R, ex19del) and T790M mt, with up to 60-fold selectivity over wild type (wt) EGFR in vitro. |
| Targets&IC50 | mutant EGFR: 0.031 μM(Ki) |
| In vitro | H1975, H3255, HCC827, A431, and HaCaT cells are maintained in RPMI media supplemented with antibiotics and 10% FBS, maintained in a 37°C, 5% CO2 humidified incubator. After an overnight incubation in 384-well plates, serial diluted compounds are transferred to cells and incubated for 3 hours. HaCaT cells are stimulated with 10 ng/mL EGF (50 ng/mL EGF for A431) for 5 minutes. Cells are lysed in 1% Triton X-100 buffer containing protease and phosphatase inhibitors. Lysates are analyzed by sandwich ELISA utilizing goat anti-EGFR capture antibody, anti-phospho-EGFR(Y1173), and anti-rabbit HRP. Signal is measured by chemiluminescent detection.(Only for Reference) |
| Synonyms | NVS-816, EGF816 |
| CAS No. | 1508250-71-2 |
| Chemical Formula | C26H31ClN6O2 |
| Molecular Weight | 495.02 |
| Solubility | DMSO: 92 mg/mL (185.9 mM) Ethanol: 92 mg/mL (185.9 mM); H2O: <1 mg/mL |
| Storage | Powder: -20°C for 2 years In solvent: -80°C for 1 year |
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