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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C25H23F3N4O2 |
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分子量 | 468.47 | CAS No. | 2097262-58-1 | |
Solubility (25°C)* | 体外 | DMSO | 94 mg/mL (200.65 mM) | |
Ethanol | 50 mg/mL (106.73 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | TVB-3664 is a potent, selective, orally active and reversible inhibitor of fatty acid synthase (FASN) with IC50 of 0.018 μM and 0.012 μM for human and mouse cell palmitate synthesis, respectively. |
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in vitro | TVB-3664 induces FASN inhibition with significantly reduced tubulin palmitoylation and mRNA expression. Disrupted microtubule organization in tumor cells is an additional consequence of FASN inhibition. TVB-3664 combined with taxane treatment enhances inhibition of in vitro tumor cell growth compared to treatmentwith either agent alone.[1] |
in vivo | In lung, ovarian, prostate, and pancreatic tumor xenograft studies, TVB-3664 and paclitaxel or docetaxel combine to inhibit xenograft tumor growth with significantly enhanced anti-tumor activity. Tumor regression is observed in 3 of 6 tumor xenograftmodels.[1] |
細胞アッセイ | 細胞株 | Calu-6 cells, A549 cells |
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濃度 | 50 nM | |
反応時間 | 48 h, 72 h | |
実験の流れ | Calu-6 cells are treated with 50 nM TVB-3664 for 48 h. Paclitaxel is added to the cell culture media to a final concentration of 6 nM. After the 2 h of incubation with paclitaxel, cells and supernatant are collected for analysis. |
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動物実験 | 動物モデル | female BALB-c-nude mice |
投薬量 | 10 mg/kg, 2.5 mg/kg | |
投与方法 | PO, IV |
De novo lipogenesis fuels adipocyte autophagosome and lysosome membrane dynamics [ Nat Commun, 2023, 14(1):1362] | PubMed: 36914626 |
Dual targeting of hepatocyte DGAT2 and stellate cell FASN alleviates nonalcoholic steatohepatitis in mice [ bioRxiv, 2023, 2023.07.05.547848] | PubMed: 37461560 |
ATP citrate lyase controls hematopoietic stem cell fate and supports bone marrow regeneration [ EMBO J, 2022, e109463] | PubMed: 35229328 |
Pharmacological inhibition of fatty acid synthesis blocks SARS-CoV-2 replication [ Nat Metab, 2021, 10.1038/s42255-021-00479-4] | PubMed: 34580494 |
Metabolomic credentialing of murine carcinogen-induced urothelial cancer [ Sci Rep, 2021, 11(1):22085] | PubMed: 34764423 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。