1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETVB-3664Cat. No.: HY-120062CAS No.: 2097262-58-1分式: CHFNO分量: 468.47作靶點: Fatty Acid Synthase (FAS)作通路: Metabolic Enzyme/Protease儲存式: Please store the product under the recommended conditions inthe COA.BIOLOGICAL ACTIVITY物活性 TVB-3

2、664具有服活性的、可逆的、有效的、選擇性的并具有物利度的脂酸合酶 (FASN) 抑制劑，其對和棕櫚酸酯合成的 IC50 值分別為 18 nM 和 12 nM?？娠@著降低微管蛋棕櫚?；?mRNA表達。IC50 & Target FASN 1 2.體外研究 TVB-3664 (0-1 M, 7 days) shows anti-tumor activity in CaCo2, HT29 and LIM2405 cell lines 1.TVB-3664 decreases viability in multiple tumor cell lines from solid and hematop

3、oietic tumor types 1.Cell Proliferation Assay 1Cell Line: CaCo2, HT29 and LIM2405 cell lines.Concentration: 0-1 M.Incubation Time: 7 days.Result: Showed anti-tumor activity.體內(nèi)研究TVB-3664 (3 mg/kg (Pt 2614 and Pt 2449PT) or 6 mg/kg (Pt 2402 and Pt 2449LM), oral gavage, daily, 4weeks) treatment leads t

4、o 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%, respectively1.1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEAnimal Model: Colorectal cancer (CRC) PDX models in NOD-SCID-IL2r

5、g-/- (NSG) mice usingspecimens collected from patients who had undergone surgery for resection of primaryCRC or CRC metastasis 1.Dosage: 3 mg/kg (Pt 2614 and Pt 2449PT) or 6 mg/kg (Pt 2402 and Pt 2449LM).Administration: Oral gavage daily for 4 weeks.Result: Led to a significant reduction in tumor vo

6、lume and tumor weight in Pt 2614, Pt 2449PT,and Pt 2402 PDX models, with an average reduction in tumor weight of 30%, 37.5% and51.5%, respectively.REFERENCES1. Zaytseva YY, et al. Preclinical evaluation of novel fatty acid synthase inhibitors in primary colorectal cancer cells and a patient-derivedx

7、enograft 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 Modelsthrough Disruption of Tubulin Palmitoylation and Microtubule Organization and FASN Inhibition-Mediated Effects on Oncogenic Signalingand Gene Expression. EBioMedicine. 2017 Feb;16:51-62.McePdfHeightCaution: Product has not been fully validated for medical applications.For resea