产品展示
SCH 900776
点击次数：217发布时间：2013/4/7 14:58:01
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
SCH 900776
上海义森生物科技有限公司
技术数据:
分子量（MW）: 376.25 
化学式: C15H18BrN7
溶解度: DMSO 60mg/mL Water <1mg/mL Ethanol 3mg/mL 纯度: >99% 稳定性: at -20℃ 2 years CAS号: 891494-63-6
生物活性
SCH 900776 is a potent ａnd functionally selective targeting cell cycle checkpoint kinase 1 （CHK1） inhibitor with IC50 of 3 nM, 0.16 ａnd 1.5 μM for CHK1, CDK2 ａnd CHK2, respectively. Checkpoint kinase 1 （CHK1） is an essential serine/threonine kinase which responds to DNA damage ａnd stalled DNA replication. CHK1 is essential for maintenance of replication fork viability during exposure to DNA antimetabolites. SCH 900776 possesses potential radiosensitization ａnd chemosensitization activities. In addition, simultaneous addition of SCH 727965 during hydroxyurea exposure also suppressed accumulation of γ-H2AX, in a dose-dependent manner. SCH 900776 reveals an approximate EC50 of 60 nM. In direct binding studies, the Kd of SCH 900776 for the CHK1 kinase domain was determined to be 2 nM, in good line with the enzymatically determined IC50. SCH 900776 is a weak inhibitor of CDK2. 4 mg/kg SCH 900776 was sufficient to induce the γ-H2AX biomarker while 8 mg/kg led to enhanced tumor pharmacodynamic ａnd regression responses relative to gemcitabine or SCH 900776 alone. Dose escalation of SCH 900776 （16 ａnd 32 mg/kg） induced incremental improvements in tumor response. In addition, combination of gemcitabine at clinically relevant levels with active doses of SCH 900776 was not associated with synergistic myelosuppression in BALB/c mice. [1] SCH 900776 is originally developed by Schering-Plough. The phase I clinical trials for SCH 900776 have been completed.
技术数据:
分子量（MW）: 376.25 化学式: C15H18BrN7
溶解度: DMSO 60mg/mL Water <1mg/mL Ethanol 3mg/mL 纯度: >99% 稳定性: at -20℃ 2 years CAS号: 891494-63-6
生物活性
SCH 900776 is a potent ａnd functionally selective targeting cell cycle checkpoint kinase 1 （CHK1） inhibitor with IC50 of 3 nM, 0.16 ａnd 1.5 μM for CHK1, CDK2 ａnd CHK2, respectively. Checkpoint kinase 1 （CHK1） is an essential serine/threonine kinase which responds to DNA damage ａnd stalled DNA replication. CHK1 is essential for maintenance of replication fork viability during exposure to DNA antimetabolites. SCH 900776 possesses potential radiosensitization ａnd chemosensitization activities. In addition, simultaneous addition of SCH 727965 during hydroxyurea exposure also suppressed accumulation of γ-H2AX, in a dose-dependent manner. SCH 900776 reveals an approximate EC50 of 60 nM. In direct binding studies, the Kd of SCH 900776 for the CHK1 kinase domain was determined to be 2 nM, in good line with the enzymatically determined IC50. SCH 900776 is a weak inhibitor of CDK2. 4 mg/kg SCH 900776 was sufficient to induce the γ-H2AX biomarker while 8 mg/kg led to enhanced tumor pharmacodynamic ａnd regression responses relative to gemcitabine or SCH 900776 alone. Dose escalation of SCH 900776 （16 ａnd 32 mg/kg） induced incremental improvements in tumor response. In addition, combination of gemcitabine at clinically relevant levels with active doses of SCH 900776 was not associated with synergistic myelosuppression in BALB/c mice. [1] SCH 900776 is originally developed by Schering-Plough. The phase I clinical trials for SCH 900776 have been completed.
技术数据:
分子量（MW）: 376.25 化学式: C15H18BrN7
溶解度: DMSO 60mg/mL Water <1mg/mL Ethanol 3mg/mL 纯度: >99% 稳定性: at -20℃ 2 years CAS号: 891494-63-6
生物活性
SCH 900776 is a potent ａnd functionally selective targeting cell cycle checkpoint kinase 1 （CHK1） inhibitor with IC50 of 3 nM, 0.16 ａnd 1.5 μM for CHK1, CDK2 ａnd CHK2, respectively. Checkpoint kinase 1 （CHK1） is an essential serine/threonine kinase which responds to DNA damage ａnd stalled DNA replication. CHK1 is essential for maintenance of replication fork viability during exposure to DNA antimetabolites. SCH 900776 possesses potential radiosensitization ａnd chemosensitization activities. In addition, simultaneous addition of SCH 727965 during hydroxyurea exposure also suppressed accumulation of γ-H2AX, in a dose-dependent manner. SCH 900776 reveals an approximate EC50 of 60 nM. In direct binding studies, the Kd of SCH 900776 for the CHK1 kinase domain was determined to be 2 nM, in good line with the enzymatically determined IC50. SCH 900776 is a weak inhibitor of CDK2. 4 mg/kg SCH 900776 was sufficient to induce the γ-H2AX biomarker while 8 mg/kg led to enhanced tumor pharmacodynamic ａnd regression responses relative to gemcitabine or SCH 900776 alone. Dose escalation of SCH 900776 （16 ａnd 32 mg/kg） induced incremental improvements in tumor response. In addition, combination of gemcitabine at clinically relevant levels with active doses of SCH 900776 was not associated with synergistic myelosuppression in BALB/c mice. [1] SCH 900776 is originally developed by Schering-Plough. The phase I clinical trials for SCH 900776 have been completed.
技术数据:
| 分子量（MW）: | 376.25 | |
|---|---|---|
| 化学式: | C15H18BrN7 | |
| 溶解度: | DMSO 60mg/mL Water <1mg/mL Ethanol 3mg/mL | |
| 纯度: | >99% | |
| 稳定性: | at -20℃ 2 years | |
| CAS号: | 891494-63-6 |
生物活性
SCH 900776 is a potent ａnd functionally selective targeting cell cycle checkpoint kinase 1 （CHK1） inhibitor with IC50 of 3 nM, 0.16 ａnd 1.5 μM for CHK1, CDK2 ａnd CHK2, respectively. Checkpoint kinase 1 （CHK1） is an essential serine/threonine kinase which responds to DNA damage ａnd stalled DNA replication. CHK1 is essential for maintenance of replication fork viability during exposure to DNA antimetabolites. SCH 900776 possesses potential radiosensitization ａnd chemosensitization activities. In addition, simultaneous addition of SCH 727965 during hydroxyurea exposure also suppressed accumulation of γ-H2AX, in a dose-dependent manner. SCH 900776 reveals an approximate EC50 of 60 nM. In direct binding studies, the Kd of SCH 900776 for the CHK1 kinase domain was determined to be 2 nM, in good line with the enzymatically determined IC50. SCH 900776 is a weak inhibitor of CDK2. 4 mg/kg SCH 900776 was sufficient to induce the γ-H2AX biomarker while 8 mg/kg led to enhanced tumor pharmacodynamic ａnd regression responses relative to gemcitabine or SCH 900776 alone. Dose escalation of SCH 900776 （16 ａnd 32 mg/kg） induced incremental improvements in tumor response. In addition, combination of gemcitabine at clinically relevant levels with active doses of SCH 900776 was not associated with synergistic myelosuppression in BALB/c mice. [1] SCH 900776 is originally developed by Schering-Plough. The phase I clinical trials for SCH 900776 have been completed.
