Cenisertib (Synonyms: AS-703569; R-763) |
Catalog No.GC35651 |
Le cénisertib (AS-703569) est un inhibiteur multi-kinase compétitif pour l'ATP qui bloque l'activité d'Aurora-kinase-A/B, ABL1, AKT, STAT5 et FLT3. Le cénisertib induit des effets inhibiteurs de croissance majeurs en bloquant l'activité de plusieurs cibles moléculaires différentes dans les mastocytes néoplasiques (MC). Le cénisertib inhibe la croissance tumorale dans les modèles de xénogreffe de tumeurs pancréatiques, mammaires, du cÔlon, ovariennes et pulmonaires et de leucémie.
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Cas No.: 871357-89-0
Sample solution is provided at 25 µL, 10mM.
Cenisertib (AS-703569) is a multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC)[1]. Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia[2]. Aurora-A Aurora-B ABL1 Akt STAT5
Cenisertib (AS-703569) (1-1000 nM; for 48 hours) induces dose-dependent inhibition of proliferation in primary neoplastic mast cells (MC) [1].Cenisertib (5-100 nM; for 24 hours) induces a substantial G2/M cell cycle arrest at low nanomolar concentrations in all MC lines[1].Cenisertib (1-1000 nM; for 24 hours)induces apoptosis in HMC-1.1, HMC-1.2, C2, and NI-1 cells in a dose-dependent manner[1].Cenisertib (5-500 nM; for 24 hours) induces cleavage of caspase 3 in both HMC-1 sub-clones as well as in C2 and NI-1 cells[1]. Cell Proliferation Assay[1] Cell Line: HMC-1.1, HMC-1.2, ROSAKIT WT, ROSAKIT D816V and MCPV-1.1 mast cells
Cenisertib (AS-703569) (orally; 7 or 10 mg/kg/day; for 3 days) significantly suppresses tumor growth. Animal Model: Female CB17 Severe Combined Immunodeficiency (SCID) mice bearing NCI-MDR tumors[2]
[1]. Peter B, et al. Drug-induced inhibition of phosphorylation of STAT5 overrides drug resistance in neoplastic mast cells. Leukemia. 2018 Apr;32(4):1016-1022. [2]. McLaughlin J, et al. Preclinical characterization of Aurora kinase inhibitor R763/AS703569 identified through an image-based phenotypic screen. J Cancer Res Clin Oncol. 2010 Jan;136(1):99-113.
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