Nazartinib (EGF816, NVS-816) is a third-generation, orally bioavailable epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) developed by Novartis, designed to selectively target mutant forms of EGFR including the T790M resistance mutation commonly found in non-small cell lung cancer (NSCLC). In preclinical studies, Nazartinib demonstrated potent inhibition of EGFR phosphorylation in cell lines harboring activating EGFR mutations (e.g., L858R, exon 19 deletions) and T790M mutations, with IC₅₀ values in the low nanomolar range (e.g., ~2–5 nM for mutant EGFR in vitro), while sparing wild-type EGFR (IC₅₀ ~500 nM or higher), suggesting a favorable therapeutic index. In xenograft models, Nazartinib significantly reduced tumor growth in EGFR T790M-positive NSCLC models.
MedKoo Cat#: 414006
Name: Nazartinib mesylate trihydrate
CAS#: 1784778-10-4 (mesylate hydrate)
Chemical Formula: C27H41ClN6O8S
Exact Mass: 644.2395
Molecular Weight: 645.17
Elemental Analysis: C, 50.27; H, 6.41; Cl, 5.49; N, 13.03; O, 19.84; S, 4.97
The following data is based on the product molecular weight 645.17 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
