Denifanstat
TVB-2640 is an orally bioavailable fatty acid synthase (FASN) inhibitor, with potential antineoplastic activity. Upon administration, TVB-2640 binds to and blocks FASN, which prevents the synthesis of palmitate needed for tumor cell growth and survival. This leads to a reduction in cell signaling, an induction of tumor cell apoptosis and the inhibition of cell proliferation in susceptible tumor cells. FASN, an enzyme responsible for the de novo synthesis of palmitic acid, is overexpressed in tumor cells and plays a key role in tumor metabolism, lipid signaling, tumor cell survival and drug resistance; tumor cells are dependent on increased fatty acid production for their enhanced metabolic needs and rapid growth.
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化学信息
| 名称 | Denifanstat |
|---|---|
| Iupac 化学名称 | 4-(1-(4-Cyclobutyl-2-methyl-5-(5-methyl-4H-1,2,4-triazol-3- yl)benzoyl)piperidin-4-yl)benzonitrile |
| 同义词 | Denifanstat; TVB2640; TVB2640; TVB 2640; Fatty Acid Synthase Inhibitor 2, FASN-IN-2 |
| 英文同义词 | Denifanstat; TVB2640; TVB2640; TVB 2640; Fatty Acid Synthase Inhibitor 2, FASN-IN-2 |
| 分子式 | C27H29N5O |
| 分子量 | 439.55 |
| Smile | N#CC1=CC=C(C2CCN(C(C3=CC(C4=NN=C(C)N4)=C(C5CCC5)C=C3C)=O)CC2)C=C1 |
| InChiKey | BBGOSBDSLYHMRA-UHFFFAOYSA-N |
| InChi | InChI=1S/C27H29N5O/c1-17-14-24(22-4-3-5-22)25(26-29-18(2)30-31-26)15-23(17)27(33)32-12-10-21(11-13-32)20-8-6-19(16-28)7-9-20/h6-9,14-15,21-22H,3-5,10-13H2,1-2H3,(H,29,30,31) |
| Cas号 | 1399177-37-7 |
| 相关CAS号 |
订购信息
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
| 外观性状 | 固体粉末 |
|---|---|
| 纯度 | 98% Min. |
| 存储 | 短期（几天到几周）为0-4摄氏度，长期（几个月）为-20摄氏度 |
| 可溶性 | 溶于DMSO |
| 处理方式 | |
| 运输条件 | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周. |
| 海关编码 |
| Targets | |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: O'Farrell M, Duke G, Crowley R, Buckley D, Martins EB, Bhattacharya D, Friedman SL, Kemble G. FASN inhibition targets multiple drivers of NASH by reducing steatosis, inflammation and fibrosis in preclinical models. Sci Rep. 2022 Sep 19;12(1):15661. doi: 10.1038/s41598-022-19459-z. PMID: 36123383; PMCID: PMC9485253.
2: Kelly W, Diaz Duque AE, Michalek J, Konkel B, Caflisch L, Chen Y, Pathuri SC, Madhusudanannair-Kunnuparampil V, Floyd J, Brenner A. Phase II Investigation of TVB-2640 (Denifanstat) with Bevacizumab in Patients with First Relapse High- Grade Astrocytoma. Clin Cancer Res. 2023 Jul 5;29(13):2419-2425. doi: 10.1158/1078-0432.CCR-22-2807. PMID: 37093199; PMCID: PMC10320469.
3: Hasan SMN, Lou JW, Keszei AFA, Dai DL, Mazhab-Jafari MT. Atomic model for core modifying region of human fatty acid synthase in complex with Denifanstat. Nat Commun. 2023 Jun 12;14(1):3460. doi: 10.1038/s41467-023-39266-y. PMID: 37308485; PMCID: PMC10258763.
