化学信息：
| 化学名 | 5-[[5-[2-(3-aminopropoxy)-6-methoxyphenyl]-1H-pyrazol-3-yl]amino]pyrazine-2-carbonitrile |
|
| 简称 | LY2606368 | |
| 别名 |
LY 2606368, LY-2606368, Prexasertib |
|
| 中文名 | N/A | |
| 化学式 | C18H19N7O2 | |
| 分子量 | 365.39 | |
| CAS号 | 1234015-52-1 | |
| 纯度 | 98% | |
| 溶剂/溶解度 |
Water<1mg/ml; DMSO4mg/ml; Ethanol<1mg/ml |
|
| 溶液配制 | 5mg加入1.37ml DMSO，或者每3.65mg加入1ml DMSO，配制成10mM溶液。SC6569-10mM用DMSO配制。 |
生物信息：
| 产品描述 | LY2606368 is a potent and selective ATP competitive inhibitor(IC50=1.5nM in SW1990 cell) of the Chk1 protein kinase. | ||||
| 信号通路 | Cell Cycle; DNA Damage | ||||
| 靶点 | Chk1 | － | － | － | － |
| IC50 | 1.5nM | － | － | － | － |
| 体外研究 | LY2606368 alone significantly inhibited the cell proliferation in a variety of pancreatic cell lines (SW1990, SU86.86, Bx-PC3, AsPC-1, CFPAC-1, Capan-2, HPAF-II) with SW1990 being the most sensitive (IC50=1.5nM). LY2606368 has been reported to inhibit Chk1 auto-phosphorylation activated by DNA damaging agents, and induce phosphorylation of H2AX, a DNA damage maker in multiple cancer cell lines in vitro. In addition, LY2606368 has demonstrated potent single agent activity and potentiates the anti-tumor activity of DNA damaging agents in vivo. Pancreatic cancer is one of the least curable cancers, with an approximate 5% overall 5-year survival for all patients. In SW1990 pancreas orthotopic model, which represents the local and metastatic growth pattern seen in pancreas cancer patients, LY2606368 treatment resulted in over 92% inhibition of primary tumor growth as well as 100% inhibition of metastasis to lymph node, spleen and intestine. The anti-tumor effect of LY2606368 treatment was further demonstrated in comparing with gemcitabine (the standard of care for pancreas cancer patient) in SW1990 orthotopic model. | ||||
| 体内研究 | N/A | ||||
| 临床实验 | N/A | ||||
| 特征 | N/A | ||||
相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
| 酶活性检测实验 | |
| 方法 | N/A |
| 细胞实验 | |
| 细胞系 | N/A |
| 浓度 | N/A |
| 处理时间 | N/A |
| 方法 | N/A |
| 动物实验 | |
| 动物模型 | N/A |
| 配制 | N/A |
| 剂量 | N/A |
| 给药方式 | N/A |
| 产品编号 | 产品名称 | 包装 |
| SC6569-10mM | LY2606368 (Chk抑制剂) | 10mM×0.2ml |
| SC6569-5mg | LY2606368 (Chk抑制剂) | 5mg |
| SC6569-25mg | LY2606368 (Chk抑制剂) | 25mg |
| — | 说明书 | 1份 |
保存条件：
-20℃保存，至少一年有效。5mg和25mg包装也可室温保存，至少6个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
