Crenigacestat (LY3039478) is an orally active Notch and γ-secretase inhibitor, with an IC50 of 1 nM in most of the tumor cell lines tested.
体外研究
Crenigacestat (100 nM) exhibits anti-cancer activity in K07074 cells (a primary mouse liver tumor cell line).
Crenigacestat (LY3039478) decreases expression of Myc and cyclin A1 (part of the NOTCH-driven proliferative signature) in murine and human model systems. Crenigacestat (LY3039478) treatment also leads to G0/G1 cell cycle arrest in CCRCC cells.
Cell Viability Assay.
Cell Line:
K07074 cells.
Concentration:
100 nM.
Incubation Time:
24-96 hours.
Result:
Effectively reduced the growth of K07074 cells.
体内研究
Crenigacestat (8 mg/kg, oral gavage three times a week) resulted in significantly increases survival and delayed tumor growth in independent cohorts of mice demonstrating in vivo efficacy in CCRCC.
Animal Model:
CCRCC xenografts were established in NOD-scid IL2R null mice with subcutaneous implantation using the 769-P cell line.
Dosage:
8 mg/kg.
Administration:
Oral gavage three times a week.
Result:
Resulted in increased overall survival when compared with vehicle control in CCRCC xenografts.
分子式
C22H23F3N4O4
分子量
464.44
CAS号
1421438-81-4
运输条件
Room temperature in continental US; may vary elsewhere.