CAS NO: | 2648641-36-3 |
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 |
生物活性 | Zotizalkib (TPX-0131) is a potent, selective, CNS-penetrant and orally active inhibitor ofwild-type ALK(IC50of 1.4 nM) andALK-resistant mutation, e.g.G1202R(IC50of 0.3 nM),L1196M(IC50of 0.3 nM). Zotizalkib has strong antitumor activities[1]. | ||||||||||||||||
IC50& Target | IC50: 1.4 nM (Wild-typr AKT); 0.2-6.6 nM (mutant ALK variants)[1] | ||||||||||||||||
体外研究 (In Vitro) | Zotizalkib potently inhibits wild-type ALK (IC50=1.4 nM) and 26 ALK resistance mutations. Zotizalkib inhibits C1156Y, E1210K/S1206C, L1198F/C1156Y, L1196M/L1198F, E1210K, L1196M, T1151M, deleted G1202, S1206R, G1202R/L1198F, F1174L, F1245C, R1275Q, and G1202R ALK mutations with IC50 values of<1 nm. zotizalkib has ic50values of 1-2 nM for the following ALK mutations: L1198F, L1152R, F1174S, T1151-L1152 insT, V1180L, G1269A, F1174C. Zotizalkib is less active against ALK mutations including I1171N, L1152P, D1203N, D1203N/E1210K, and G1269S, with IC50values of 2-7 nM[1]. | ||||||||||||||||
体内研究 (In Vivo) | Zotizalkib (2-10 mg/kg; p.o.; twice a day; for 2 weeks) treatment at 2 mg/kg, 5 mg/kg, and 10 mg/kg resulted in dose-dependent tumor growth inhibition (TGI) of 64%, 120%, and 200% (complete regression), respectively[1].
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Clinical Trial | |||||||||||||||||
分子量 | 447.41 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C21H20F3N5O3 | ||||||||||||||||
CAS 号 | 2648641-36-3 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 25 mg/mL(55.88 mM;ultrasonic and warming and heat to 60℃) 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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