TVB-3166

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-3166 诱导细胞凋亡并抑制体内异种移植肿瘤生长。 TVB-3166 是一种可逆、选择性脂肪酸合酶抑制剂（生化 FASN 和细胞棕榈酸酯合成的 IC50 分别为 42 nM 和 81 nM）。

TVB-3166 induces apoptosis and inhibits in-vivo xenograft tumor growth. TVB-3166 is a reversible and selective fatty acid synthase inhibitor (IC50s: 42 nM and 81 nM for biochemical FASN and cellular palmitate synthesis, respectively).(In Vitro):TVB-3166 (0.2 μM; 48 hours) inhibits β-catenin pathway signal transduction and transcriptional activity. TVB-3166 (0.02 or 0.20 μM; 7 days) suppresses palmitate synthesis and tumor cell viability in a dose-dependent manner. TVB-3166 (0.001-10 μM; 24 hours) induces cell death in CALU-6 non-small-cell lung tumor cells (cellular IC50: 0.10 μM) . (In Vivo):TVB-3166 (Oral gavage; 30-100 mg/kg/day) has the concentration is approximately 3-fold higher in plasma than the tumor. TVB-3166 (Oral gavage; 30-100 mg/kg/day) inhibits xenograft tumor growth. The 100 and 30 mg/kg groups had plasma and tumor concentrations of 7 and 2.9 μM, respectively .

Cell Proliferation Assay Cell Line:CALU-6 tumor cells Concentration:0.001, 0.01, 0.1, 1, 10 μMIncubation Time:24 hoursResult:Caused cell death in CALU-6 non-small-cell lung tumor cells with a cellular IC50 value of 0.10 μM.Cell Viability Assay Cell Line:90 different tumor cell lines (such as CALU-6 NSCLC cell line, NCI-H1975 NSCLC cell line) Concentration:0.02 or 0.20 μM Incubation Time:7 days Result:Dose-dependent induction of cell death was observed in all tumor cell lines.Western Blot Analysis Cell Line:COLO-205 and A549 cells Concentration:0.2 μM Incubation Time:48 hours Result:Inhibited β-catenin pathway signal transduction and transcriptional activity.

Animal Model:Female BALB-c-nude miceDosage:30, 60, or 100 mg/kg Administration:Oral gavage; once daily Result:Inhibited xenograft tumor growth.Animal Model:Female BALB-c-nude miceDosage: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.

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Apoptosis

Apoptosis

Bacterial

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1533438-83-3

384.483

C24H24N4O

>98% (HPLC)

In Vitro:?DMSO : 62.5 mg/mL (162.56 mM)

Cc1n[nH]c(c1C)-c1cc(C(=O)N2CC(C2)c2ccc(cc2)C#N)c(C)cc1C

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(-20℃)

With Ice Pack

≥ 2 years