化学信息：
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化学名
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5-[[5-[2-(3-aminopropoxy)-6-methoxyphenyl]-1H-pyrazol-3-yl]amino]pyrazine-2-carbonitrile
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简称
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LY2606368
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别名
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LY 2606368, LY-2606368, Prexasertib
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中文名
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N/A
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化学式
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C18H19N7O2
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分子量
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365.39
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CAS号
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1234015-52-1
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纯度
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98%
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溶剂/溶解度
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Water<1mg/ml; DMSO4mg/ml; Ethanol<1mg/ml
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溶液配制
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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。
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生物信息：
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产品描述
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LY2606368 is a potent and selective ATP competitive inhibitor(IC50=1.5nM in SW1990 cell) of the Chk1 protein kinase.
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信号通路
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Cell Cycle; DNA Damage
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靶点
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Chk1
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－
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－
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－
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－
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IC50
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1.5nM
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－
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－
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－
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－
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体外研究
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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.
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体内研究
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N/A
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临床实验
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N/A
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特征
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N/A
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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)：
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酶活性检测实验
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方法
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N/A
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细胞实验
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细胞系
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N/A
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浓度
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N/A
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处理时间
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N/A
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方法
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N/A
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动物实验
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动物模型
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N/A
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配制
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N/A
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剂量
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N/A
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给药方式
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N/A
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产品编号
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产品名称
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包装
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SC6569-10mM
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LY2606368 (Chk抑制剂)
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10mM×0.2ml
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SC6569-5mg
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LY2606368 (Chk抑制剂)
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5mg
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SC6569-25mg
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LY2606368 (Chk抑制剂)
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25mg
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—
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说明书
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1份
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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。
注意事项：
本产品仅限于专业人员的科学研究用，不得用于临床诊断或治疗，不得用于食品或药品，不得存放于普通住宅内。
为了您的安全和健康，请穿实验服并戴一次性手套操作。
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