TVB-3166
目录号: PL14894 纯度: ≥99%
CAS No. :1533438-83-3
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中文名称
TVB-3166
英文名称
TVB-3166
英文别名
4-(1-(5-(3,4-Dimethyl-1H-pyrazol-5-yl)-2,4-dimethylbenzoyl)azetidin-3-yl)benzonitrile;FASN-IN-3;4-{1-[5-(4,5-Dimethyl-2H-pyrazol-3-yl)-2,4-dimethyl-benzoyl]-azetidin-3-yl}-benzonitrile;4-(1-(5-(4,5-Dimethyl-1H-pyrazol-3-yl)-2,4-dimethylbenzoyl)azetidin-3-yl)benzonitrile;4-[1-[5-(4,5-dimethyl-1H-pyrazol-3-yl)-2,4-dimethylbenzoyl]azetidin-3-yl]benzonitrile;BDBM244633;s3576;US94285;TVB-3166
Cas No.
1533438-83-3
分子式
C24H24N4O
分子量
384.47
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
TVB-3166 是一种口服有效,可逆和选择性脂肪酸合成酶 (FASN) 抑制剂,对于 FASN 和细胞棕榈酸酯合成的 IC50 分别为 42 nM 和 81 nM。TVB-3166 诱导细胞凋亡,并抑制体内异种移植肿瘤的生长。
生物活性
TVB-3166 is an orally-available, reversible, and selective fatty acid synthase (FASN) inhibitor with IC 50 s 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.
性状
Solid
IC50 & Target[1][2]
IC50: 42 nM (FASN) and 81 nM (cellular palmitate synthesis)
体外研究(In Vitro)
TVB-3166 (0.001-10 μM; 24 hours) causes cell death in CALU-6 non-small-cell lung tumor cells with a cellular IC50 value of 0.10 μM.
TVB-3166 (0.02 or 0.20 μM; 7 days) inhibits palmitate synthesis and tumor cell viability in a dose-dependent manner.
TVB-3166 (0.2 μM; 48 hours) inhibits β-catenin pathway signal transduction and transcriptional activity.
has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
TVB-3166 (Oral gavage; 30-100 mg/kg/day) inhibits xenograft tumor growth.
TVB-3166 (Oral gavage; 30-100 mg/kg/day) has the concentration is 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.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Ventura R, et al. Inhibition of de novo Palmitate Synthesis by Fatty Acid Synthase Induces Apoptosis in Tumor Cells by Remodeling Cell Membranes, Inhibiting Signaling Pathways, and Reprogramming Gene Expression. EBioMedicine. 2015 Jul 2;2(8):808-24.
溶解度数据
In Vitro: DMSO : 62.5 mg/mL (162.56 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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