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A-674563
点击次数：232发布时间：2013/4/7 15:33:45
更新日期：2022/8/19 17:45:40
所 在 地：美洲
产品型号：
优质供应
详细内容
A-674563
上海义森生物科技有限公司
技术数据:
分子量（MW）: 358.44 
化学式: C22H22N4O
溶解度: DMSO 72mg/mL Water 72mg/mL Ethanol 18mg/mL 纯度: >99% 稳定性: at -20℃ 2 years CAS号: 552325-73-2
生物活性
A-674563 is a potent selective protein kinase B/Akt inhibitor with an IC50 of 14 nM. A-674563 also shows inhibitory activity against PKA ａnd CDK2 with IC50 of 16 ａnd 46 nM, respectively. While promising efficacy was observed in vivo, A-674563 indicated significantly effects on depolarization of purkinje fiber in an in vitro assay ａnd severe CV toxicity （e.g. hypotension） in vivo. An X-ray structure of A-674563 bound to protein kinase A, which has 80% homology with Akt in the kinase domain, suggested the phenyl group is not tightly bound in the ligand-protein complex. The Akt inhibitor A-674563 displayed proliferation of tumor cells with an EC50 of 0.4 μM. When given in combination, A-674563 enhanced the efficacy of paclitaxel in a PC-3 xenograft model.[1][2]
技术数据:
分子量（MW）: 358.44 化学式: C22H22N4O
溶解度: DMSO 72mg/mL Water 72mg/mL Ethanol 18mg/mL 纯度: >99% 稳定性: at -20℃ 2 years CAS号: 552325-73-2
生物活性
A-674563 is a potent selective protein kinase B/Akt inhibitor with an IC50 of 14 nM. A-674563 also shows inhibitory activity against PKA ａnd CDK2 with IC50 of 16 ａnd 46 nM, respectively. While promising efficacy was observed in vivo, A-674563 indicated significantly effects on depolarization of purkinje fiber in an in vitro assay ａnd severe CV toxicity （e.g. hypotension） in vivo. An X-ray structure of A-674563 bound to protein kinase A, which has 80% homology with Akt in the kinase domain, suggested the phenyl group is not tightly bound in the ligand-protein complex. The Akt inhibitor A-674563 displayed proliferation of tumor cells with an EC50 of 0.4 μM. When given in combination, A-674563 enhanced the efficacy of paclitaxel in a PC-3 xenograft model.[1][2]
技术数据:
分子量（MW）: 358.44 化学式: C22H22N4O
溶解度: DMSO 72mg/mL Water 72mg/mL Ethanol 18mg/mL 纯度: >99% 稳定性: at -20℃ 2 years CAS号: 552325-73-2
生物活性
A-674563 is a potent selective protein kinase B/Akt inhibitor with an IC50 of 14 nM. A-674563 also shows inhibitory activity against PKA ａnd CDK2 with IC50 of 16 ａnd 46 nM, respectively. While promising efficacy was observed in vivo, A-674563 indicated significantly effects on depolarization of purkinje fiber in an in vitro assay ａnd severe CV toxicity （e.g. hypotension） in vivo. An X-ray structure of A-674563 bound to protein kinase A, which has 80% homology with Akt in the kinase domain, suggested the phenyl group is not tightly bound in the ligand-protein complex. The Akt inhibitor A-674563 displayed proliferation of tumor cells with an EC50 of 0.4 μM. When given in combination, A-674563 enhanced the efficacy of paclitaxel in a PC-3 xenograft model.[1][2]
技术数据:
| 分子量（MW）: | 358.44 | |
|---|---|---|
| 化学式: | C22H22N4O | |
| 溶解度: | DMSO 72mg/mL Water 72mg/mL Ethanol 18mg/mL | |
| 纯度: | >99% | |
| 稳定性: | at -20℃ 2 years | |
| CAS号: | 552325-73-2 |
生物活性
A-674563 is a potent selective protein kinase B/Akt inhibitor with an IC50 of 14 nM. A-674563 also shows inhibitory activity against PKA ａnd CDK2 with IC50 of 16 ａnd 46 nM, respectively. While promising efficacy was observed in vivo, A-674563 indicated significantly effects on depolarization of purkinje fiber in an in vitro assay ａnd severe CV toxicity （e.g. hypotension） in vivo. An X-ray structure of A-674563 bound to protein kinase A, which has 80% homology with Akt in the kinase domain, suggested the phenyl group is not tightly bound in the ligand-protein complex. The Akt inhibitor A-674563 displayed proliferation of tumor cells with an EC50 of 0.4 μM. When given in combination, A-674563 enhanced the efficacy of paclitaxel in a PC-3 xenograft model.[1][2]
