EGF816 (mesylate)
EGF816 (mesylate) Basic information
- Product Name:
- EGF816 (mesylate)
- Synonyms:
-
- EGF816 (mesylate)
- CS-2105
- EGF816 mesylate (EGF-816 mesylate
- Nazartinib mesylate)
- EGF-816 MESYLATE;NAZARTINIB MESYLATE
- N-[7-chloro-1-[(3R)-1-[(E)-4-(dimethylamino)but-2-enoyl]azepan-3-yl]benzimidazol-2-yl]-2-methylpyridine-4-carboxamide
- Nazartinib trifluoroacetate salt
- Nazartinib mesylate (EGF81)
- CAS:
- 1508250-72-3
- MF:
- C27H35ClN6O5S
- MW:
- 591.12
- Mol File:
- 1508250-72-3.mol
EGF816 (mesylate) Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
EGF816 (mesylate) Usage And Synthesis
Uses
Nazartinib mesylate (EGF816 mesylate) is a novel, covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min?1 on EGFR(L858R/790M) mutant, respectively.
in vivo
In H1975 mouse xenograft model, Nazartinib (EGF816; 50 and 20 mg/kg or 25 mg/kg, p.o.) demonstrates dose-dependent efficacy with near complete tumor cells regression at the highest dose tested (50 mg/kg)[1]. In H1975 mouse model, Nazartinib (EGF816; 10 mg/kg, p.o.) induces tumor growth inhibition with a T/C (tumor/control volume) of 29%, and when doses are 30 and 100 mg/kg, tumor regressions are achieved (T/C, ?61% and ?80%, respectively). In the H3255 xenograft model, Nazartinib (30 mg/kg, p.o.) shows significant antitumor activity. Antiproliferative activity of Nazartinib on 89 lung cancer cell lines indicates that Nazartinib selectively inhibits cell lines containing EGFR with catalytic domain mutations[2].
IC 50
EGFRL858R/T790M: 31 nM (Ki)
References
[1] Lelais G, et al. Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T79 DOI:10.1021/acs.jmedchem.5b01985
[2] Jia Y, et al. EGF816 Exerts Anticancer Effects in Non-Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor. Cancer Res. 2016 Mar 15;76(6):1591-602 DOI:10.1158/0008-5472.CAN-15-2581
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