CAS NO: | 2137030-98-7 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | Ensartinib dihydrochloride (X-396 dihydrochloride) is a potent and dualALK/METinhibitor withIC50s of<0.4 nM and 0.74 nM, respectively. | ||||||||||||||||
IC50& Target | IC50:<0.4 nM (ALK), 0.74 nM (MET)[1] | ||||||||||||||||
体外研究 (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 harboringEML4-ALKE13;A20 (IC50: 15 nM). Ensartinib dihydrochloride is also potent in H2228 lung cancer cells harboringEML4-ALKE6a/b; A20 (IC50: 45 nM). Furthermore, X-376 is potent in SUDHL-1 lymphoma cells harboringNPM-ALK(IC50: 9 nM)[1]. | ||||||||||||||||
体内研究 (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 Cmaxof 7.19 μM[1]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 634.36 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C26H29Cl4FN6O3 | ||||||||||||||||
CAS 号 | 2137030-98-7 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | ||||||||||||||||
溶解性数据 | In Vitro: DMSO : 35.71 mg/mL(56.29 mM;Need ultrasonic) H2O : 33.33 mg/mL(52.54 mM;Need ultrasonic) 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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