LY2606368 (Chk抑制剂)

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。

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

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

KL569-10mM

LY2606368 (Chk抑制剂)

10mM×0.2ml

KL6569-5mg

LY2606368 (Chk抑制剂)

5mg

KL6569-25mg

LY2606368 (Chk抑制剂)

25mg

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说明书

1份