B2402374计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥99% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
避光,-20°C储存,充氩。超低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Targets
CXCR4 (Cell-free) 0.079 nM
In vitro
In human lymphoma U937 cells expressing endogenous CXCR4, LY2510924 inhibits SDF-1-induced cell migration with IC50 value of 0.26 nmol/L 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 reveal that LY2510924 has no apparent agonist activity. LY2510924 has no inhibitory activities against other chemokine receptors including CCR1, CCR2, CXCR2, and CXCR3 at the concentrations tested. Similarly, there is no activity observed among serotonin, dopamine, and opioid receptors.
LY2510924 has acceptable in vivo stability and a pharmacokinetic profile similar to a typical small-molecular inhibitor in preclinical species. LY2510924 shows dose-dependent inhibition of tumor growth in human xenograft models developed with non-Hodgkin lymphoma, renal cell carcinoma, lung, and colon cancer cells that express functional CXCR4. In MDA-MB-231, a breast cancer metastatic model, LY2510924 inhibits tumor metastasis by blocking migration/homing process of tumor cells to the lung and by inhibiting cell proliferation after tumor cell homing. LY2510924 has a dramatically improved in vivo stability with a half-life of 3 to 5 hours in preclinical species and 9.16 hours in humans at the recommended phase II dose.
Cell Research(from reference)
Cell lines：U937 cells
Incubation Time：2.5 h
规格
英文别名
L-Lysinamide,L-phenylalanyl-L-tyrosyl-N6-(1-methylethyl)-L-lysyl-D-arginyl-3-(2-naphthalenyl)-L-alanylglycyl-D-α-glutamyl-N6-(1-methylethyl)-,(7→1)-lactam
规格或纯度
≥99%
英文名称
LY2510924 TFA salt
生化机理
LY2510924 是一种强效的选择性 CXCR4 拮抗剂，能特异性阻断 SDF-1 与 CXCR4 的结合，IC50 值为 0.079 nmol/L，并能抑制 SDF-1 诱导的 GTP 结合，Kb 值为 0.38 nmol/L。
储存条件
避光,-20°C储存,充氩
运输条件
超低温运输
作用类型
抑制剂
纯度
≥99%
名称和识别符
分子类型
小分子
分子量
1189.45(free basis)
技术文档
高级数据
化学和物理性质
溶解性
Solubility (25°C) In vitro Water: 100 mg/mL (84.07 mM);
敏感性
对光线敏感；对湿度敏感
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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