恩沙替尼
中文名称 | 恩沙替尼 |
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中文同义词 | 恩沙替尼;恩沙替尼(X-376);ALK抑制剂(ENSARTINIB);恩沙替尼(X 396);(R)-6-氨基-5-(1-(2,6-二氯-3-氟苯基)乙氧基)-N-(4-(4-甲基哌嗪-1-羰基)苯基)哒嗪-3-甲酰胺;ENSARTINIB (ALK/MET抑制剂) |
英文名称 | X-376 |
英文同义词 | X-376;X-396;6-Amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-[(4-methyl-1-piperazinyl)carbonyl]phenyl]-3-pyridazinecarboxamide;Ensartinib;(R)-6-amino-5-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-N-(4-(4-methylpiperazine-1-carbonyl)phenyl)pyridazine-3-carboxamide;6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-(4-methylpiperazine-1-carbonyl)phenyl]pyridazine-3-carboxamide;CS-1720;3-Pyridazinecarboxamide, 6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-[(4-methyl-1-piperazinyl)carbonyl]phenyl]- |
CAS号 | 1365267-27-1 |
分子式 | C25H25Cl2FN6O3 |
分子量 | 547.41 |
EINECS号 | |
相关类别 | 抑制剂;小分子抑制剂;科研试剂;细胞生物学试剂;成熟工艺 |
Mol文件 | 1365267-27-1.mol |
结构式 |
恩沙替尼 性质
沸点 | 695.1±55.0 °C(Predicted) |
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密度 | 1.428±0.06 g/cm3(Predicted) |
储存条件 | Store at -20°C |
溶解度 | 乙醇:13.0(最大浓度 mg/mL);23.75(最大浓度 mM) |
形态 | 结晶固体 |
酸度系数(pKa) | 10.70±0.70(Predicted) |
颜色 | 白色至米白色 |
恩沙替尼治疗较常见的副作用包括皮疹、瘙痒、水肿、贫血等,大多数为1-2级,程度轻微,发生率最高的3级或以上明显副作用为皮疹(6%)和颜面部水肿(4%)。恩沙替尼治疗过程中较常见的实验室检查结果异常,包括肝酶两项、γ-谷氨酰转肽酶、碱性磷酸酶、血清淀粉酶和血肌酐升高。
X-376是ALK抑制剂,对治疗非小细胞性肺癌有潜在疗效。Target | Value |
ALK
() |
The ability of X-376 to inhibit the growth of different cancer cell lines harboring ALK fusions or point mutations is tested. X-376 is potent in H3122 lung cancer cells harboring EML4-ALK E13;A20 (IC 50 : 77 nM). X-376 is also potent in H2228 lung cancer cells harboring EML4-ALK E6a/b; A20 (IC 50 : 57 nM). Furthermore, X-376 is potent in SUDHL-1 lymphoma cells harboring NPM-ALK (IC 50 : 32 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 142 nM, 150 nM, 15.137 μM and 3.062 μM, respectively.
The effects of X-376 in vivo against H3122 xenografts are examined. A pharmacokinetic study reveals that X-376 shows substantial bioavailability and moderate half-lives in vivo. Nude mice harboring H3122 xenografts are treated with X-376 at 50 mg/kg bid. X-376 significantly delays the growth of tumors compared to vehicle alone. In the xenograft experiments, X-376 appears well-tolerated in vivo. Mouse weight is unaffected by X-376 treatment. Drug-treated mice appear healthy and do not display any signs of compound related toxicity. To further assess potential side effects of X-376, additional systemic toxicity and toxico-kinetic studies are performed in Sprague Dawley (SD) rats. Following 10 days of repeated oral administration of X-376 at 25, 50, 100 mg/kg in SD rats, all animals survive to study termination. The no significant toxicity (NST) levels are determined to be 50 mg/kg for X-376. At NST levels, X-376 achieves an AUC of 41 μM×hr and a C max of 5.04 μM.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/04/30 | HY-16590 | 恩沙替尼 X-376 | 1365267-27-1 | 5mg | 1700元 |
2024/04/30 | HY-16590 | 恩沙替尼 X-376 | 1365267-27-1 | 10mM * 1mLin DMSO | 2047元 |