TVB-3664

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

TVB-3664 显着降低微管蛋白棕榈酰化和 mRNA 表达。 TVB-3664 是一种可逆且高生物利用度的脂肪酸合酶抑制剂（对于人和小鼠细胞棕榈酸酯合成，IC50 分别为 18 nM 和 12 nM）。

TVB-3664 significantly decreases tubulin palmitoylation and mRNA expression. TVB-3664 is a reversible and highly bioavailable fatty acid synthase inhibitor (IC50: 18 nM and 12 nM for human and mouse cell palmitate synthesis, respectively).(In Vitro):TVB-3664 reduces viability in multiple tumor cell lines from solid and hematopoietic tumor types. TVB-3664 (0-1 μM, 7 days) displays anti-tumor activity in CaCo2, HT29, and LIM2405 cell lines .(In Vivo):In Pt 2614, Pt 2449PT, and Pt 2402 PDX models, TVB-3664 (3 mg/kg or 6 mg/kg, oral gavage, daily, 4 weeks) treatment leads to a significant reduction in tumor volume and tumor weight, with an average reduction in tumor weight of 30%, 37.5%, and 51.5%, respectively .

Cell Proliferation Assay Cell Line:CaCo2, HT29 and LIM2405 cell lines.Concentration:0-1 μM.Incubation Time:7 days.Result:Showed anti-tumor activity.

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.

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Metabolic Enzyme/Protease

Fatty Acid Synthase

Drug Metabolite

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2097262-58-1

468.48

C25H23F3N4O2

>98% (HPLC)

In Vitro:?DMSO : 10 mg/mL (21.35 mM)

COCc1nc([nH]c1-c1cc(C(=O)N2CC(C2)c2ccc(cc2)C#N)c(C)cc1C)C(F)(F)F

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(-20℃)

With Ice Pack

≥ 2 years