LY2510924 - CXCR 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELY2510924Cat. No.: HY-12488CAS No.: 1088715-84-7分式: CHNO分量: 1189.45作靶点: CXCR作通路: GPCR/G Protein; Immunology/Inflammation储存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 125 mg/mL (105.09 mM)* means so

2、luble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 0.8407 mL 4.2036 mL 8.4072 mL5 mM 0.1681 mL 0.8407 mL 1.6814 mL10 mM 0.0841 mL 0.4204 mL 0.8407 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，

3、当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.25 mg/mL (1.89 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.25 mg/mL (1.89 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2

4、.25 mg/mL (1.89 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 LY2510924有效，选择性的 CXCR4 拮抗剂；阻SDF-1结合CXCR4，IC50值为0.079 nM。IC50 & Target SDF-1-CXCR4 SDF-1-CXCR479.7 pM (IC50) 49.5 pM (Ki)体外研究 LY2510924 specifically blocks SDF-1 binding to CXCR4 with IC50 value

5、 of 0.079 nM, and inhibits SDF-1induced GTP binding with Kb value of 0.38 nM. In human lymphoma U937 cells expressing endogenousCXCR4, LY2510924 inhibits SDF-1induced cell migration with IC50 value of 0.26 nM and inhibits SDF-1/CXCR4-mediated intracellular signaling. LY2510924 exhibits a concentrati

6、on-dependent inhibition of SDF-1stimulated phospho-ERK and phospho-Akt in tumor cells. Biochemical and cellular analyses reveals thatLY2510924 has no apparent agonist activity 1. LY2510924 chiefly inhibits the proliferation of AML cells withlittle induction of cell death and reduces protection again

7、st chemotherapy by stromal cells 2.体内研究 LY2510924 specifically blocks SDF-1 binding to CXCR4 with IC50 value of 0.079 nM, and inhibits SDF-1induced GTP binding with Kb value of 0.38 nM. In human lymphoma U937 cells expressing endogenousCXCR4, LY2510924 inhibits SDF-1induced cell migration with IC50

8、value of 0.26 nM and inhibits SDF-1/CXCR4-mediated intracellular signaling. LY2510924 exhibits a concentration-dependent inhibition of SDF-1stimulated phospho-ERK and phospho-Akt in tumor cells. Biochemical and cellular analyses reveals thatLY2510924 has no apparent agonist activity 1. LY2510924 chi

9、efly inhibits the proliferation of AML cells withlittle induction of cell death and reduces protection against chemotherapy by stromal cells 2.PROTOCOLKinase Assay LY2510924 specifically blocks SDF-1 binding to CXCR4 with IC50 value of 0.079 nM, and inhibits SDF-1induced GTP binding with Kb value of

10、 0.38 nM. In human lymphoma U937 cells expressing endogenousCXCR4, LY2510924 inhibits SDF-1induced 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-1stimulated phospho-ERK and phospho-A

11、kt in tumor cells. Biochemical and cellular analyses reveals thatLY2510924 has no apparent agonist activity 1. LY2510924 chiefly inhibits the proliferation of AML cells withlittle induction of cell death and reduces protection against chemotherapy by stromal cells 2.MCE has not independently confirm

12、ed the accuracy of these methods. They are for reference only.Animal Mice: SCID female mice are injected intravenously with MDA-MB-231 cells, and are treated subcutaneouslyAdministration 1 with vehicle (1PBS) or 3 mg/kg of LY2510924 formulated in 1PBS. Group 1 and 2 animals receive vehicleor 3 mg/kg

13、 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 dayafter tumor cell injection. After treatment, lung tissues are fixed in 10% neutral-buffered forma

14、lin for at least24 hours and lung lobes are present in histologic sections 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE户使本产品发表的科研献 Nat Commun. 2018 Jul 4;9(1):2612. Cancer Gene Ther. 2019 Apr 26.See

15、 more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Peng SB, et al. Identification of LY2510924, a novel cyclic peptide CXCR4 antagonist that exhibits antitumor activities in solid tumor andbreast 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 withchemotherapy. B