化學(xué)名

5-[[5-[2-(3-aminopropoxy)-6-methoxyphenyl]-1H-pyrazol-3-yl]amino]pyrazine-2-carbonitrile

簡(jiǎn)稱

LY2606368

別名

LY 2606368, LY-2606368, Prexasertib

中文名

N/A

化學(xué)式

C₁₈H₁₉N₇O₂

分子量

365.39

CAS號(hào)

1234015-52-1

純度

98%

溶劑/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。

產(chǎn)品描述

LY2606368 is a potent and selective ATP competitive inhibitor(IC50=1.5nM in SW1990 cell) of the Chk1 protein kinase.

信號(hào)通路

Cell Cycle; DNA Damage

靶點(diǎn)

Chk1

－

－

－

－

IC50

1.5nM

－

－

－

－

體外研究

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.

體內(nèi)研究

N/A

臨床實(shí)驗(yàn)

N/A

特征

N/A

酶活性檢測(cè)實(shí)驗(yàn)

方法

N/A

細(xì)胞實(shí)驗(yàn)

細(xì)胞系

N/A

濃度

N/A

處理時(shí)間

N/A

方法

N/A

動(dòng)物實(shí)驗(yàn)

動(dòng)物模型

N/A

配制

N/A

劑量

N/A

給藥方式

N/A

產(chǎn)品編號(hào)

產(chǎn)品名稱

包裝

KL569-10mM

LY2606368 (Chk抑制劑)

10mM×0.2ml

KL6569-5mg

LY2606368 (Chk抑制劑)

5mg

KL6569-25mg

LY2606368 (Chk抑制劑)

25mg

—

說(shuō)明書(shū)

1份