| Company Name: |
SPIRO PHARMA |
| Tel: |
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| Email: |
eric_feng1954@126.com |
| Company Name: |
Musechem |
| Tel: |
+1-800-259-7612 |
| Email: |
info@musechem.com |
EGF816 (mesylate) manufacturers
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| | 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 | | EINECS: | | | Product Categories: | | | 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 min1 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 |
| | EGF816 (mesylate) Preparation Products And Raw materials |
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