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编 号:F259497
分子式:C25H23F3N4O2
分子量:468.47
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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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25mg
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50mg
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生物活性:
TVB-3664 is an orally available, reversible, potent, selective and highly bioavailable fatty acid synthase (FASN) inhibitor, with IC50 values of 18 nM and 12 nM for human and mouse cell palmitate synthesis, respectively. TVB-3664 significantly reduces tubulin palmitoylation and mRNA expression.

体内研究:
TVB-3664 (3 mg/kg (Pt 2614 和 Pt 2449PT) 或 6 mg/kg (Pt 2402 和 Pt 2449LM),口服强饲,每天,4 周) 处理导致肿瘤体积和肿瘤重量显著减少、Pt 2614, Pt 2449PT 和 Pt 2402 PDX 模型,平均肿瘤重量分别减少 30%、37.5% 和 51.5%。Animal Model:Colorectal cancer (CRC) PDX models in NOD-SCID-IL2rg-/- (NSG) mice using specimens collected from patients who had undergone surgery for resection of primary CRC or CRC metastasis.
Dosage:3 mg/kg (Pt 2614 and Pt 2449PT) or 6 mg/kg (Pt 2402 and Pt 2449LM).
Administration:Oral gavage daily for 4 weeks.
Result:Led to a significant reduction in tumor volume and tumor weight in Pt 2614, Pt 2449PT, and Pt 2402 PDX models, with an average reduction in tumor weight of 30%, 37.5% and 51.5%, respectively.

体外研究:
TVB-3664 (0-1 μM,7 天) 在 CaCo2、HT29 和 LIM2405 细胞系中表现出抗肿瘤活性。 TVB-3664 降低多种肿瘤细胞系的活力来自实体瘤和造血肿瘤。
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