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.
体外研究
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.
体内研究
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.
Animal Model:
Non-obese diabetic-severe combined immunodeficient (NOD–SCID) mice implanted with MM.1S cells.
Dosage:
100 mg/kg and 200 mg/kg.
Administration:
Oral gavage daily.
Result:
Led to a significant dose-dependent inhibition of tumor growth.
分子式
C24H23F4N7O3
分子量
533.48
CAS号
1959551-26-8
运输条件
Room temperature in continental US; may vary elsewhere.