Nazartinib (EGF816) | mutant EGFR inhibitor

Chemical Structure : EGF816

CAS No.: 1508250-71-2

EGF816 (EGF-816, Nazartinib)

Catalog No.: PC-43273Not 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 for EGFR (L858R/790M), respectively.

Packing	Price	Stock
5 mg	$88	In stock
10 mg	$128	In stock
25 mg	$218	In stock
50 mg	$358	In stock
100 mg		Get quote

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Biological Activity

EGF816 (Nazartinib) is a potent, irreversible, mutant-selective EGFR inhibitor with Ki and Kinact of 31 nM and 0.222 min-1 for EGFR (L858R/790M), respectively.
EGF816 (Nazartinib) 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.
EGF816 (Nazartinib) potently inhibits the most common EGFR mutations L858R, Ex19del, and T790M in vitro.
EGF816 (Nazartinib) 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	495.0163
Formula	C26H31ClN6O2
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	DMSO: ≥ 242 mg/mL
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-

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.

EGF816 (EGF-816, Nazartinib)

Biological Activity

Physicochemical Properties

References

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