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Chemical Structure : EGF816
CAS No.: 1508250-71-2
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 | Quantity |
|---|---|---|---|
| 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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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.
| M.Wt | 495.0163 | |
| Formula | C26H31ClN6O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
DMSO: ≥ 242 mg/mL |
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| 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- |
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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.
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