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编 号:F754348
分子式:C21H20F3N5O3
分子量:447.41
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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生物活性:
Zotizalkib (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). Zotizalkib has strong antitumor activities.

体内研究:
Zotizalkib (2-10 mg/kg;口服;每天两次;持续 2 周) 2mg /kg、5mg /kg 和10mg /kg 的剂量依赖性肿瘤生长抑制(TGI)分别为64%、120% 和 200%(完全回归)。Animal Model:Female SCID/beige mice (5-8 weeks old) bearing Ba/F3 cells
Dosage:2 mg/kg, 5 mg/kg, and 10 mg/kg
Administration:p.o.; twice a day; for 2 weeks
Result:Caused complete tumor regression in ALK mutation-dependent xenograft models.

体外研究:
Zotizalkib 有效抑制野生型 ALK (IC50=1.4 nM) 和 26 种 ALK 耐药突变。 Zotizalkib 抑制 C1156Y、E1210K/S1206C、L1198F/C1156Y、L1196M/L1198F、E1210K、L1196M、T1151M、缺失的 G1202、S1206R、G1202R/L1198F、F1174L、F1245C、R12 75Q 和 G1202R ALK 突变,IC50 值 Zotizalkib 相关抗体:
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