生物活性 靶点 体外研究 体内研究
ChemicalBook  CAS数据库列表  561.44

561.44

561.44,1370651-20-9,结构式
561.44
  • CAS号:1370651-20-9
  • 英文名:C26H27Cl2FN6O3
  • 中文名:561.44
  • CBNumber:CB83151688
  • 分子式:C26H27Cl2FN6O3
  • 分子量:561.44
  • MOL File:1370651-20-9.mol
561.44化学性质
  • 储存条件 :Store at -20°C
  • 溶解度 :Soluble in DMSO

561.44性质、用途与生产工艺

  • 生物活性 Ensartinib (X-396) 是一种有效的双重的 ALK/MET 抑制剂,IC50 分别 <0.4 nM 和 0.74 nM。
  • 靶点

    MET

    0.74 nM (IC 50 )

  • 体外研究

    The ability of Ensartinib (X-396) to inhibit the growth of different cancer cell lines harboring ALK fusions or point mutations is tested. Ensartinib is potent in H3122 lung cancer cells harboring EML4-ALK E13;A20 (IC 50 : 15nM). Ensartinib is also potent in H2228 lung cancer cells harboring EML4-ALK E6a/b; A20 (IC 50 : 45 nM). Furthermore, X-376 is potent in SUDHL-1 lymphoma cells harboring NPM-ALK (IC 50 : 9 nM). X-376 also inhibits SY5Y neuroblastoma cells harboring ALK F1174L, MKN-45 gastric carcinoma cells harboring MET dependent, HepG2 cells and PC-9 lung cancer cell lines harboring EGFR exon 19 del with IC 50 s of 68 nM, 156 nM, 9.644 μM and 2.989 μM, respectively.

  • 体内研究

    The effects of Ensartinib (X-396) in vivo against H3122 xenografts are examined. A pharmacokinetic study reveals that Ensartinib shows substantial bioavailability and moderate half-lives in vivo. Nude mice harboring H3122 xenografts are treated with Ensartinib at 25mg/kg bid. Ensartinib significantly delays the growth of tumors compared to vehicle alone. In the xenograft experiments, Ensartinib appears well-tolerated in vivo. Mouse weight is unaffected by Ensartinib treatment. Drug-treated mice appear healthy and do not display any signs of compound related toxicity. To further assess potential side effects of Ensartinib, additional systemic toxicity and toxico-kinetic studies are performed in Sprague Dawley (SD) rats. Following 10 days of repeated oral administration of Ensartinib 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 80mg/kg for Ensartinib. At NST levels, Ensartinib achieves an AUC of 66 μM×hr and a C max of 7.19 μM.

561.44上下游产品信息
上游原料
下游产品
561.44生产厂家
  • 公司名称:上海喀露蓝科技有限公司
  • 联系电话:18149758185 18149758185
  • 电子邮件:sales-cpd@caerulumpharma.com
  • 国家:中国
  • 产品数:3466
  • 优势度:58