在線訂購 免費訂購熱線:021-59541103 021-60443211
標(biāo)簽:Cenisertib
聯(lián)系人:高小姐
電話:021-59541103 021-60443211
手機(jī):13585831301
Q Q: 3004967995
Email:3004967995@qq.com
詳細(xì)地址:上海嘉定區(qū)嘉羅公路1661
化學(xué)性質(zhì):
規(guī)格 | 100mg |
CAS | 871357-89-0 |
別名 | N/A |
化學(xué)名 | N/A |
分子式 | C24H30FN7O |
分子量 | 451.54 |
溶解度 | DMSO: 250 mg/mL (553.66 mM) |
儲存條件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
產(chǎn)品描述:
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.
特別提醒:
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原創(chuàng)作者:上海莼試生物技術(shù)有限公司
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普票匯款信息
賬 戶 名:上海生物
開 戶 行:中國銀行山東省分行營業(yè)部
賬 號:2169 2341 6278