EGF816 mesylate (Nazartinib mesylate)

Chemical Structure : EGF816 mesylate

Catalog No.: PC-43274Not For Human Use, Lab Use Only.

EGF816 (Nazartinib) is a potent, irreversible, mutant-selective EGFR inhibitor with Ki and Kinact of 31 nM and 0.222 min-1, respectively.

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Biological Activity

Nazartinib (EGF816) mesylate is a potent, irreversible, mutant-selective EGFR inhibitor with Ki and Kinact of 31 nM and 0.222 min-1, respectively.
Nazartinib (EGF816) shows potent inhibition of pEGFR levels in H3255, HCC827, and H1975 with EC50 of 5, 1, and 3 nM, which harbor the L858R, Ex19del, and L858R/T790M mutations, respectively, inhibitscell proliferation with EC50 of 9, 11, and 25 nM, but not the WT EGFR-containing patient-derived cell lines.
Nazartinib (EGF816) potently inhibits the most common EGFR mutations L858R, Ex19del, and T790M in vitro.
Nazartinib (EGF816) causes tumor regressions in vivo in several patient-derived xenograft models, also demonstrates antitumor activity in exon 20 insertion mutant model.

Physicochemical Properties

M.Wt	591.122
Formula	C27H35ClN6O5S
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	4-Pyridinecarboxamide, N-[7-chloro-1-[(3R)-1-[(2E)-4-(dimethylamino)-1-oxo-2-buten-1-yl]hexahydro-1H-azepin-3-yl]-1H-benzimidazol-2-yl]-2-methyl-, methanesulfonate (1:1)

References

1. Lelais G, et al. J Med Chem. 2016 Jul 28;59(14):6671-89.

2. Jia Y, et al. Cancer Res. 2016 Mar 15;76(6):1591-602.

3. Liao BC, et al. Lung Cancer. 2017 Aug;110:7-13.