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AT9283
点击次数:369发布时间:2013/4/7 18:04:41
更新日期:2022/8/19 17:45:40
所 在 地:美洲
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详细内容
AT9283
上海义森生物科技有限公司
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
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]
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
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]
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
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]
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 |
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]