产品
编 号:F156520
分子式:C22H23F3N4O4
分子量:464.44
产品类型
结构图
CAS No: 1421438-81-4
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产品详情
生物活性:
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.
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.