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产品价格:电议      采购度:1297      原产地:美洲
发布时间:2022/4/27 14:23:02 所属地区:国外 国外
简要描述:
Ensartinib dihydrochloride (X-396 dihydrochloride) 是一种有效的双重的 ALK/MET 抑制剂,IC50 分别 < nM 和 nM。
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CAS No. : 2137030-98-7
MCE 站:Ensartinib dihydrochloride
产品活性:Ensartinib dihydrochloride (X-396 dihydrochloride) 是一种有效的双重的 ALK/MET 抑制剂,IC50 分别 <0.4 nM 和 0.74 nM。
研究领域:Protein Tyrosine Kinase/RTK
作用靶点:ALK | c-Met/HGFR
In Vitro: Ensartinib (X-396) dihydrochloride is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively. Ensartinib dihydrochloride is potent in H3122 lung cancer cells harboring EML4-ALK E13;A20 (IC50: 15 nM). Ensartinib dihydrochloride is also potent in H2228 lung cancer cells harboring EML4-ALK E6a/b; A20 (IC50: 45 nM). Furthermore, X-376 is potent in SUDHL-1 lymphoma cells harboring NPM-ALK (IC50: 9 nM).
In Vivo: Ensartinib (X-396) dihydrochloride shows substantial bioavailability and moderate half-lives in vivo. Nude mice harboring H3122 xenografts are treated with Ensartinib dihydrochloride at 25 mg/kg bid. Ensartinib dihydrochloride significantly delays the growth of tumors compared to vehicle alone. In the xenograft experiments, Ensartinib dihydrochloride appears well-tolerated in vivo. Mouse weight is unaffected by Ensartinib dihydrochloride treatment. Drug-treated mice appear healthy and do not display any signs of compound related toxicity. To further assess potential side effects of Ensartinib dihydrochloride, additional systemic toxicity and toxico-kinetic studies are performed in Sprague Dawley (SD) rats. Following 10 days of repeated oral administration of Ensartinib dihydrochloride at 20, 40, 80 mg/kg in SD rats, all animals survive to study termination. The no significant toxicity (NST) levels are determined to be 80 mg/kg for Ensartinib dihydrochloride. At NST levels, Ensartinib dihydrochloride achieves an AUC of 66 μM×hr and a Cmax of 7.19 μM.
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更新时间:2024/1/2 10:22:49
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