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.
For research use only. We do not sell to patients.
Chemical Information
| Name | Denifanstat |
|---|---|
| Iupac Chemical Name | 4-(1-(4-Cyclobutyl-2-methyl-5-(5-methyl-4H-1,2,4-triazol-3- yl)benzoyl)piperidin-4-yl)benzonitrile |
| Synonyms | Denifanstat; TVB2640; TVB2640; TVB 2640; Fatty Acid Synthase Inhibitor 2, FASN-IN-2 |
| Molecular Formula | C27H29N5O |
| Molecular Weight | 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 Number | 1399177-37-7 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Solid powder |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| HS Code |
| Targets | |
|---|---|
| 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.
Chemical Structure
