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LY2510924
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LY2510924图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
LY2510924 是一种有效的选择性 CXCR4 拮抗剂;阻断 SDF-1 与 CXCR4 的结合,IC50 为 0.079 nM。

Kinase experiment:

LY2510924 specifically blocks SDF-1 binding to CXCR4 with IC50 value of 0.079 nM, and inhibits SDF-1–induced GTP binding with Kb value of 0.38 nM. In human lymphoma U937 cells expressing endogenous CXCR4, LY2510924 inhibits SDF-1–induced cell migration with IC50 value of 0.26 nM and inhibits SDF-1/CXCR4-mediated intracellular signaling. LY2510924 exhibits a concentration-dependent inhibition of SDF-1–stimulated phospho-ERK and phospho-Akt in tumor cells. Biochemical and cellular analyses reveals that LY2510924 has no apparent agonist activity[1]. LY2510924 chiefly inhibits the proliferation of AML cells with little induction of cell death and reduces protection against chemotherapy by stromal cells[2].

Animal experiment:

Mice: SCID female mice are injected intravenously with MDA-MB-231 cells, and are treated subcutaneously with vehicle (1×PBS) or 3 mg/kg of LY2510924 formulated in 1×PBS. Group 1 and 2 animals receive vehicle or 3 mg/kg of LY2510924 twice daily for days with treatment beginning on one day before tumor cell injection. Group 3 animals receive 3 mg/kg of LY2510924 15 twice daily for 13 days with treatment beginning one day after tumor cell injection. After treatment, lung tissues are fixed in 10% neutral-buffered formalin for at least 24 hours and lung lobes are present in histologic sections[1].

产品描述

LY2510924 is a potent and selective CXCR4 antagonist; blocks SDF-1 binding to CXCR4 with an IC50 of 0.079 nM.

LY2510924 specifically blocks SDF-1 binding to CXCR4 with IC50 value of 0.079 nM, and inhibits SDF-1-induced GTP binding with Kb value of 0.38 nM. In human lymphoma U937 cells expressing endogenous CXCR4, LY2510924 inhibits SDF-1-induced cell migration with IC50 value of 0.26 nM and inhibits SDF-1/CXCR4-mediated intracellular signaling. LY2510924 exhibits a concentration-dependent inhibition of SDF-1-stimulated phospho-ERK and phospho-Akt in tumor cells. Biochemical and cellular analyses reveals that LY2510924 has no apparent agonist activity[1]. LY2510924 chiefly inhibits the proliferation of AML cells with little induction of cell death and reduces protection against chemotherapy by stromal cells[2].

LY2510924 specifically blocks SDF-1 binding to CXCR4 with IC50 value of 0.079 nM, and inhibits SDF-1-induced GTP binding with Kb value of 0.38 nM. In human lymphoma U937 cells expressing endogenous CXCR4, LY2510924 inhibits SDF-1-induced cell migration with IC50 value of 0.26 nM and inhibits SDF-1/CXCR4-mediated intracellular signaling. LY2510924 exhibits a concentration-dependent inhibition of SDF-1-stimulated phospho-ERK and phospho-Akt in tumor cells. Biochemical and cellular analyses reveals that LY2510924 has no apparent agonist activity[1]. LY2510924 chiefly inhibits the proliferation of AML cells with little induction of cell death and reduces protection against chemotherapy by stromal cells[2].

References:
[1]. Peng SB, et al. Identification of LY2510924, a novel cyclic peptide CXCR4 antagonist that exhibits antitumor activities in solid tumor and breast cancer metastatic models. Mol Cancer Ther. 2015 Feb;14(2):480-90.
[2]. Cho BS, et al. Antileukemia activity of the novel peptidic CXCR4 antagonist LY2510924 as monotherapy and in combination with chemotherapy. Blood. 2015 Jul 9;126(2):222-32.