Cenisertib-AS-703569-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECenisertibCat. No.: HY-13072CAS No.: 871357-89-0Synonyms: AS-703569; R-763分式: CHFNO分量: 451.54作靶點: Aurora Kinase; Bcr-Abl; Akt; STAT; FLT3作通路: Cell Cycle/DNA Damage; Epigenetics; Protein Tyrosine Kinase/RTK; PI3K/Akt/mTOR; JAK/ST

2、AT Signaling; Stem Cell/Wnt儲存式: Please store the product under the recommended conditions inthe COA.BIOLOGICAL ACTIVITY物活性 Cenisertib (AS-703569)種多激酶抑制劑，可抑制 Aurora-kinase-A/B，ABL1，AKT，STAT5, FLT3 的活性。 Cenisertib 通過抑制腫瘤肥細胞 (MC) 中種不同分靶標(biāo)的活性抑制其長。 Cenisertib 抑制異種移植模型中胰腺癌，乳腺癌，結(jié)腸癌， 巢癌和肺癌以及病的腫瘤長。IC50 & Targ

3、et Aurora-A Aurora-B ABL1 AktSTAT5體外研究Cenisertib (AS-703569) (1-1000 nM; for 48 hours) induces dose-dependent inhibition of proliferation inprimary neoplastic mast cells (MC) 1.Cenisertib (5-100 nM; for 24 hours) induces a substantial G2/M cell cycle arrest at low nanomolarconcentrations in all MC l

4、ines 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 inC2 and NI-1 cells 1.Cell Proliferation Assay 1Cell Line: HMC-1.1,

5、HMC-1.2, ROSAKIT WT, ROSAKIT D816V and MCPV-1.1 mast cells1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEConcentration: 1, 5, 10, 50, 100, 500, 1000 nMIncubation Time: 48 hoursResult: Induced dose-dependent inhibition of proliferation in primary neoplastic MC.Cell Cycle Analysis 1Cell Line: HMC-1.

6、1, HMC-1.2, C2 and NI-1 cellsConcentration: 5, 10, 50, 100 nMIncubation Time: 24 hoursResult: Induced a substantial G2/M cell cycle arrest at low nanomolar concentrations in all MClines.Apoptosis Analysis 1Cell Line: HMC-1.1, HMC-1.2, C2 and NI-1 cellsConcentration: 1, 5, 10, 50, 100, 500, 1000 nMIn

7、cubation Time: 24 hoursResult: Induced apoptosis in HMC-1.1, HMC-1.2, C2, and NI-1 cells in a dose-dependentmanner.Western Blot Analysis 1Cell Line: HMC-1.1, HMC-1.2, C2 and NI-1 cellsConcentration: 50, 100, 500 nMIncubation Time: 24 hoursResult: Induced cleavage of caspase 3 in both HMC-1 sub-clone

8、s as well as in C2 and NI-1cells.體內(nèi)研究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-MDRtumors 2Dosage: 7 and 10 mg/kgAdministration: Orally; daily; for 3 days2/3 M

9、aster of Small Molecules 您邊的抑制劑師www.MedChemEResult: Suppressed significantly tumor growth.REFERENCES1. Peter B, et al. Drug-induced inhibition of phosphorylation of STAT5 overrides drug resistance in neoplastic mast cells. Leukemia. 2018Apr;32(4):1016-1022.2. McLaughlin J, et al. Preclinical characterization of Aurora kinase inhibitor R763/AS703569 identified through an image-based phenotypicscreen. J Cancer Res Clin Oncol. 2010 Jan;136(1):99-113.McePdfHeightCaution: Product has not been fully validated f