LY2510924 - CXCR 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELY2510924Cat. No.: HY-12488CAS No.: 1088715-84-7分式: CHNO分量: 1189.45作靶點: CXCR作通路: GPCR/G Protein; Immunology/Inflammation儲存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 125 mg/mL (105.09 mM)* means so

2、luble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，

3、當天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.25 mg/mL (1.89 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.25 mg/mL (1.89 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2

4、.25 mg/mL (1.89 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 LY2510924有效，選擇性的 CXCR4 拮抗劑；阻SDF-1結(jié)合CXCR4，IC50值為0.079 nM。IC50 & Target SDF-1-CXCR4 SDF-1-CXCR479.7 pM (IC50) 49.5 pM (Ki)體外研究 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.體內(nèi)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 您邊的抑制劑師www.MedChemE戶使本產(chǎn)品發(fā)表的科研獻 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