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AT9283

点击次数:369发布时间:2013/4/7 18:04:41

AT9283

更新日期:2022/8/19 17:45:40

所 在 地:美洲

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简单介绍:AT9283技术数据:分子量(MW): 381.43 化学式: C19H23N7O2 溶解度: DMSO 76mg/mL Water <1mg/mL Ethanol 38mg/mL 纯度: >99% 稳定性: at -20℃ 2 years CAS号: 896466-04-9, 896466-57-2 ((±)-Lactic acid), 896466-61-8 (HCl), 896466-55-0 (methanesulfonate

相关标签:AT9283 896466-04-9 

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AT9283             
                     
            
上海义森生物科技有限公司

技术数据:

分子量(MW): 381.43 AT9283 Chemical Structure
化学式:

C19H23N7O2

溶解度: DMSO 76mg/mL   Water <1mg/mL   Ethanol 38mg/mL
纯度: >99%
稳定性: at -20℃ 2 years
CAS号: 896466-04-9, 896466-57-2 ((±)-Lactic acid), 896466-61-8 (HCl), 896466-55-0 (methanesulfonate

生物活性

 

AT9283 is a small molecule a multi-targeted c-ABL, JAK2, Aurora A and B inhibitor with of 4, 1.2, 1.1 and approximate 3 nM for Bcr-Abl(T3151), Jak2 and Jak3, aurora A and B, respectively. AT9283 inhibited growth and survival of multiple solid tumor cell lines and was efficacious in mouse xenograft models. AT9283-treatment resulted in endoreduplication and ablation of serine-10 histone H3 phosphorylation in both cells and tumor samples. AT9283 demonstrated in vivo efficacy in mouse xenograft models and is currently under evaluation in phase I clinical trial. AT9283 showed potent antiproliferative activity on cells transformed by wild-type BCR-ABL and BCR-ABL/T315I. AT9283 inhibited proliferation in a panel of BaF3 and human BCR-ABL+ cell lines both sensitive and resistant to imatinib because of a variety of mechanisms. In BCR-ABL+ cells, inhibition of substrates of both BCR-ABL (signal transducer and activator of transcription-5) and Aurora B (histone H3) at physiologically achievable concentrations was confirmed. [1][2][3]

 

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