产品
编 号：F622826
分子式：C24H24N4O
分子量：384.47
分子式：C24H24N4O
分子量：384.47
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
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10mg
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50mg
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100mg
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结构图
CAS No: 1533438-83-3
产品详情
生物活性：
TVB-3166 is an orally-available, reversible, and selective fatty acid synthase (FASN) inhibitor with IC50s of 42 nM and 81 nM for biochemical FASN and cellular palmitate synthesis, respectively. TVB-3166 induces apoptosis, and inhibits in-vivo xenograft tumor growth.
体内研究：
TVB-3166 (口服强饲法；30-100 mg/kg/天) 抑制异种移植肿瘤的生长。 TVB-3166 (口服强饲法；30-100 mg/kg/day) 在血浆中的浓度比在肿瘤中的浓度高约 3 倍。100 和 30 mg/kg 组的血浆和肿瘤浓度分别为 7 和 2.9 μM。Animal Model:Female BALB-c-nude mice
Dosage:30, 60, or 100 mg/kg
Administration:Oral gavage; once daily
Result:Inhibited xenograft tumor growth.
Animal Model:Female BALB-c-nude mice
Dosage:30, 60, or 100 mg/kg (Pharmacokinetic Study)
Administration:Oral gavage; once daily
Result:The concentration was approximately 3-fold higher in plasma than tumor. The 100 and 30 mg/kg groups had plasma and tumor concentrations of 7 and 2.9 μM, respectively.
体外研究：
TVB-3166 (0.001-10 μM；24 小时) 导致 CALU-6 非小细胞肺肿瘤细胞死亡，细胞 IC50 值为 0.10 μM。 TVB-3166 (0.02 或 0.20 μM；7 天) 以剂量依赖性方式抑制棕榈酸酯合成和肿瘤细胞活力。 TVB-3166 (0.2 μM；48 小时) 抑制 β-catenin 通路信号转导和转录活性。
TVB-3166 is an orally-available, reversible, and selective fatty acid synthase (FASN) inhibitor with IC50s of 42 nM and 81 nM for biochemical FASN and cellular palmitate synthesis, respectively. TVB-3166 induces apoptosis, and inhibits in-vivo xenograft tumor growth.
体内研究：
TVB-3166 (口服强饲法；30-100 mg/kg/天) 抑制异种移植肿瘤的生长。 TVB-3166 (口服强饲法；30-100 mg/kg/day) 在血浆中的浓度比在肿瘤中的浓度高约 3 倍。100 和 30 mg/kg 组的血浆和肿瘤浓度分别为 7 和 2.9 μM。Animal Model:Female BALB-c-nude mice
Dosage:30, 60, or 100 mg/kg
Administration:Oral gavage; once daily
Result:Inhibited xenograft tumor growth.
Animal Model:Female BALB-c-nude mice
Dosage:30, 60, or 100 mg/kg (Pharmacokinetic Study)
Administration:Oral gavage; once daily
Result:The concentration was approximately 3-fold higher in plasma than tumor. The 100 and 30 mg/kg groups had plasma and tumor concentrations of 7 and 2.9 μM, respectively.
体外研究：
TVB-3166 (0.001-10 μM；24 小时) 导致 CALU-6 非小细胞肺肿瘤细胞死亡，细胞 IC50 值为 0.10 μM。 TVB-3166 (0.02 或 0.20 μM；7 天) 以剂量依赖性方式抑制棕榈酸酯合成和肿瘤细胞活力。 TVB-3166 (0.2 μM；48 小时) 抑制 β-catenin 通路信号转导和转录活性。
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