LY2606368 dihydrochloride

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抑制剂描述：

产品名称：LY2606368 dihydrochloride

产品别名：见爱必信官网

英文别名：LY2606368 dihydrochloride

靶点：Chk

CAS：1234015-54-3

纯度：98%

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

LY2606368 2Hcl is a potent and selective ATP competitive inhibitor(IC50=1.5 nM in SW1990 cell) of the Chk1 protein kinase.

溶解性：DMSO : ≥ 31 mg/mL (70.73 mM)

体外研究：

In nonclinical studies, LY2606368 induced DNA damage as measured by replication catastrophe and increases in pH2A.X, a marker of double-stranded DNA breaks. Treatment of cells with LY2606368 results in the rapid appearance of TUNEL and pH2AX-positive double-stranded DNA breaks in the S-phase cell population. In a functional assay, LY2606368 potently abrogated the G2–M checkpoint activated by doxorubicin in p53-deficient HeLa cells with an EC50 of 9 nmol/L. LY2606368 was broadly antiproliferative with IC50 values typically 1,000 nmol/L. LY2606368 requires CDC25A and CDK2 to cause DNA damage.

体内研究：LY2606368 inhibited tumor growth in cancer xenografts as monotherapy and in combination with other agents. In an orthotopic SKOV3 ovarian cancer model, LY2606368 was shown to inhibit the growth of primary tumors and significantly reduce the incidence of metastases and ascites accumulation. LY2606368 also demonstrated efficacy in an SW1990 orthotopic pancreatic cancer model resulting in a 92% inhibition of primary tumor growth and the elimination of metastases to the lymphnode, spleen, and intestine.

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