产品描述
FT671 is a non-covalent and selective inhibitor of USP7 (IC50: 52 nM) It also binds to the USP7 catalytic domain (Kd: 65 nM).
体外活性
FT671 causes the degradation of N-Myc and upregulation of p53 in the neuroblastoma cell line IMR-32. FT671 increases p53 protein levels in HCT116 or bone osteosarcoma (U2OS) cell lines, leading to the induction of p53 target genes including BBC3 (which encodes PUMA), CDKN1A (p21), RPS27L (S27L) and MDM2. FT671 also stabilizes p53 in the MM.1S multiple myeloma cell line, which correlates with increased MDM2 ubiquitination and leads to the expression of p53 target genes.
体内活性
FT671 is well-to related even at high doses. FT671 (100 mg/kg and 200 mg/kg, oral gavage, daily) treatment in mice causes an obviously dose-dependent inhibition of tumor growth.
Cas No.
1959551-26-8
分子式
C24H23F4N7O3
分子量
533.48
储存和溶解度
DMSO:50 mg/mL (93.72 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years