For research use only. Not for therapeutic Use.
FT671 is a potent, non-covalent and selective USP7 inhibitor with an IC50 of 52 nM and binds to the USP7 catalytic domain with a Kd of 65 nM.<br>FT671 increases p53 protein levels in HCT116 or bone osteosarcoma (U2OS) cell lines, leading to induction of p53 target genes including BBC3 (which encodes PUMA), CDKN1A (p21), RPS27L (S27L) and MDM2. FT671 leads to the degradation of N-Myc and upregulation of p53 in the neuroblastoma cell line IMR-32. FT671 also stabilizes p53 in the MM.1S multiple myeloma cell line, which correlates with increased MDM2 ubiquitination and leads to expression of p53 target genes[1].<br>FT671 (100 mg/kg and 200 mg/kg, Oral gavage, daily) treatment in mice leads to a significant dose-dependent inhibition of tumor growth. And FT671 is well-torelated even at high doses[1].
| Catalog Number | I020325 |
| CAS Number | 1959551-26-8 |
| Molecular Formula | C₂₄H₂₃F₄N₇O₃ |
| Purity | ≥95% |
| Reference | [1]. Turnbull AP, et al. Molecular basis of USP7 inhibition by selective small-molecule inhibitors. Nature. 2017 Oct 26;550(7677):481-486. |
