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 selectivefatty acid synthase (FASN)inhibitor withIC50s of 42 nM and 81 nM for biochemical FASN and cellular palmitate synthesis, respectively. TVB-3166 inducesapoptosis, and inhibits in-vivo xenograft tumor growth[1]. |
| IC50& Target | IC50: 42 nM (FASN) and 81 nM (cellular palmitate synthesis)[1] |
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 IC50value of 0.10 μM[1].
TVB-3166 (0.02 or 0.20 μM; 7 days) inhibits palmitate synthesis and tumor cell viability in a dose-dependent manner[1].
TVB-3166 (0.2 μM; 48 hours) inhibits β-catenin pathway signal transduction and transcriptional activity[1].
Cell Proliferation Assay[1] | Cell Line: | CALU-6 tumor cells | | Concentration: | 0.001, 0.01, 0.1, 1, 10 μM | | Incubation Time: | 24 hours | | Result: | Caused cell death in CALU-6 non-small-cell lung tumor cells with a cellular IC50value of 0.10 μM. |
Cell Viability Assay[1] | 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[1] | 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. |
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体内研究
(In Vivo) | TVB-3166 (Oral gavage; 30-100 mg/kg/day) inhibits xenograft tumor growth[1].
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[1].
| Animal Model: | Female BALB-c-nude mice[1] | | Dosage: | 30, 60, or 100 mg/kg | | Administration: | Oral gavage; once daily | | Result: | Inhibited xenograft tumor growth. |
| Animal Model: | Female BALB-c-nude mice[1] | | Dosage: | 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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| 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 | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 62.5 mg/mL(162.56 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.6010 mL | 13.0049 mL | 26.0098 mL | | 5 mM | 0.5202 mL | 2.6010 mL | 5.2020 mL | | 10 mM | 0.2601 mL | 1.3005 mL | 2.6010 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.41 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 2.08 mg/mL (5.41 mM); Suspended solution; Need ultrasonic
此方案可获得 2.08 mg/mL (5.41 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.41 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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