上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
TPX-0131 纯度: ≥95.0%
TPX-0131 是一种有效、选择性、CNS 渗透性和口服活性的野生型 ALK 抑制剂 (IC50 为 1.4 nM) 和 ALK 抗性突变,例如 G1202R (IC50 为 0.3 nM)、L1196M (IC50 为 0.3 nM)。TPX-0131 具有很强的抗肿瘤活性。
TPX-0131 Chemical Structure
CAS No. : 2648641-36-3
规格 | 价格 | 是否有货 | 数量 |
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5 mg | ¥4900 | In-stock | |
10 mg | ¥7500 | In-stock | |
25 mg | ¥14500 | In-stock | |
50 mg | 询价 | ||
100 mg | 询价 |
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TPX-0131 相关产品
•相关化合物库:
- Drug Repurposing Compound Library Plus
- Clinical Compound Library Plus
- Bioactive Compound Library Plus
- Kinase Inhibitor Library
- Protein Tyrosine Kinase Compound Library
- Anti-Cancer Compound Library
- Clinical Compound Library
- Drug Repurposing Compound Library
- Orally Active Compound Library
- Anti-Lung Cancer Compound Library
生物活性 |
TPX-0131 is a potent, selective, CNS-penetrant and orally active inhibitor of wild-type ALK (IC50 of 1.4 nM) and ALK-resistant mutation, e.g. G1202R (IC50 of 0.3 nM), L1196M (IC50 of 0.3 nM). TPX-0131 has strong antitumor activities[1]. |
IC50 & Target |
IC50: 1.4 nM (Wild-typr AKT); 0.2-6.6 nM (mutant ALK variants)[1] |
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体外研究 (In Vitro) |
TPX-0131 potently inhibits wild-type ALK (IC50 = 1.4 nM) and 26 ALK resistance mutations. TPX-0131 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. tpx0131 has ic50 values of 1-2 nM for the following ALK mutations: L1198F, L1152R, F1174S, T1151-L1152 insT, V1180L, G1269A, F1174C. TPX-0131 is less active against ALK mutations including I1171N, L1152P, D1203N, D1203N/E1210K, and G1269S, with IC50 values of 2-7 nM[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
TPX-0131 (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]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
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Clinical Trial |
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分子量 |
447.41 |
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Formula |
C21H20F3N5O3 |
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CAS 号 |
2648641-36-3 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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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°C) 配制储备液
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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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参考文献 |
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