TVB-3664
目录号: PL14890 纯度: ≥99%
CAS No. :2097262-58-1
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中文名称
TVB-3664
英文名称
TVB-3664
英文别名
s8563;4-[1-[5-[5-(Methoxymethyl)-2-(trifluoromethyl)-1H-imidazol-4-yl]-2,4-dimethylbenzoyl]azetidin-3-yl]b;TVB-3664
Cas No.
2097262-58-1
分子式
C25H23F3N4O2
分子量
468.47
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
TVB-3664 是具有口服活性的、可逆的、有效的、选择性的并具有高生物利用度的脂肪酸合酶 (FASN) 抑制剂,其对人和老鼠棕榈酸酯合成的 IC50 值分别为 18 nM 和 12 nM。可显著降低微管蛋白棕榈酰化和 mRNA表达。
生物活性
TVB-3664 is an orally available, reversible, potent, selective and highly bioavailable fatty acid synthase (FASN) inhibitor, with IC 50 values of 18 nM and 12 nM for human and mouse cell palmitate synthesis, respectively. TVB-3664 significantly reduces tubulin palmitoylation and mRNA expression.
性状
Solid
IC50 & Target[1][2]
FASN.
体外研究(In Vitro)
TVB-3664 (0-1 μM, 7 days) shows anti-tumor activity in CaCo2, HT29 and LIM2405 cell lines.
TVB-3664 decreases viability in multiple tumor cell lines from solid and hematopoietic tumor types. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation Assay
体内研究(In Vivo)
TVB-3664 (3 mg/kg (Pt 2614 and Pt 2449PT) or 6 mg/kg (Pt 2402 and Pt 2449LM), oral gavage, daily, 4 weeks) treatment leads 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. 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]. Zaytseva YY, et al. Preclinical evaluation of novel fatty acid synthase inhibitors in primary colorectal cancer cells and a patient-derived xenograft model of colorectal cancer. Oncotarget. 2018 May 15;9(37):24787-24800.
[2]. Heuer TS, et al. FASN Inhibition and Taxane Treatment Combine to Enhance Anti-tumor Efficacy in Diverse Xenograft Tumor Models through Disruption of Tubulin Palmitoylation and Microtubule Organization and FASN Inhibition-Mediated Effects on Oncogenic Sign
溶解度数据
In Vitro: DMSO : 10 mg/mL (21.35 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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