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1370651-20-9

中文名稱 561.44
英文名稱 C26H27Cl2FN6O3
CAS 1370651-20-9
分子式 C26H27Cl2FN6O3
分子量 561.44
MOL 文件 1370651-20-9.mol
更新日期 2024/12/02 08:46:17
1370651-20-9 結(jié)構(gòu)式 1370651-20-9 結(jié)構(gòu)式

基本信息

中文別名
愛沙替尼
英文別名
561.44
C26H27Cl2FN6O3
Ensartinib (X-396)
X396
X-396
X 396
ENSARTINIB

3-Pyridazinecarboxamide, 6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-[[(3R,5S)-3,5-dimethyl-1-piperazinyl]carbonyl]phenyl]-

物理化學(xué)性質(zhì)

儲存條件-20°C儲存
溶解度溶于二甲基亞砜

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H315-H319-H335

常見問題列表

生物活性
Ensartinib (X-396) 是一種有效的雙重的 ALK/MET 抑制劑,IC50 分別 <0.4 nM 和 0.74 nM。
靶點

MET

0.74 nM (IC 50 )

體外研究

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.

體內(nèi)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.

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