LY2510924 is an inhibitor of CXC chemokine receptor 4 (CXCR4), with potential antineoplastic activity. Upon subcutaneous administration, LY2510924 binds to the chemokine receptor CXCR4, thereby preventing CXCR4 binding to its ligand, stromal derived factor-1 (SDF-1), and subsequent receptor activation.
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产品名称 | CXCR1 ↓ ↑ | CXCR2 ↓ ↑ | CXCR4 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Reparixin | ✔ | 99%+ | |||||||||||||||||
SB225002 |
+++
CXCR2, IC50: 22 nM |
99%+ | |||||||||||||||||
Plerixafor |
++
CXCR4, IC50: 44 nM |
99% | |||||||||||||||||
AMD 3465 6HBr | ✔ | 98% | |||||||||||||||||
WZ811 |
++++
CXCR4, EC50: 0.3 nM |
99% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Through binding with CC- and CXC-chemokines, CCR and CXCR, the subsets of the chemokine receptor family can trigger an intracellular signal transduction cascade, thus mediating the recruitment of immune cells to the inflammation or infection sites and implicated in several immuno-related disease states, organogenesis, angiogenesis and tumor growth and metastasis. LY2510924 is a potent and selective CXCR4 inhibitor with IC50 value of 0.079nM for blocking SDF-1α binding to CXCR4. LY2510924 could completely inhibit SDF-1-mediated GTP binding with Kb value of 0.38nM. Selective inhibition by LY2510924 of SDF-1-induced migration of U937 cells can be achieved in a concentration-dependent manner with IC50 of 0.26nM. As prediction, the SDF-1- and CXCR4-mediated cell signaling, including p-ERK and p-AKT, can be inhibited by LY2510924 at concentration of 3.3nM and 0.33nM in HeLa cells, as well as IC50 values of 1.4 and 1.2nM, respectively, in Namalwa cells expressing high level of CXCR4. Subcutaneous injection with 3mg/kg LY2510924, BID, for 7 days, significantly inhibit the tumor growth of an NHL Namalwa xenograft model. Antitumor growth activities of LY2510924 can be also observed at dose of 2mg/kg or 5mg/kg in solid cancer xenograft models, RCC A-498 and A549 xenografts. Subcutaneous injection with 3mg/kg LY2510924 twice daily for 13 or 15 days inhibited breast cancer metastasis in the MDA-MB-231 model due to blocking migration/homing process of tumor cells to reduce the colony numbers of lung metastasis, as well as inhibiting cell proliferation to reduce the size of the colonies after tumor cell homing to the lung[1]. |
作用机制 | LY2510924 can occupy the binding pocket and possess ligand-receptor interactions with CXCR4 residues.[1] |
Dose | Mice: 0.06 mg/kg - 5 mg/kg[2] (s.c.) |
Administration | s.c. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT01439568 | Extensive Stage Small Cell Lun... 展开 >>g Carcinoma 收起 << | Phase 2 | Completed | - | United States, Colorado ... 展开 >> For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Denver, Colorado, United States, 80218 United States, Florida For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Fort Myers, Florida, United States, 33916 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Orlando, Florida, United States, 32804 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Pensacola, Florida, United States, 32503 United States, Illinois For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Chicago, Illinois, United States, 60637 United States, Maryland For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Bethesda, Maryland, United States, 20817 United States, Missouri For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Springfield, Missouri, United States, 65804 United States, Nebraska For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Omaha, Nebraska, United States, 68114 United States, Ohio For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Cincinnati, Ohio, United States, 45242 United States, South Carolina For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Greenville, South Carolina, United States, 29605 United States, Tennessee For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Chattanooga, Tennessee, United States, 37404 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Memphis, Tennessee, United States, 38120 For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Nashville, Tennessee, United States, 37203 United States, Texas For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Fort Worth, Texas, United States, 76104 United States, Virginia For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Richmond, Virginia, United States, 23230 收起 << |
NCT01391130 | Metastatic Clear Cell Renal Ce... 展开 >>ll Carcinoma 收起 << | Phase 2 | Terminated(Study Terminated du... 展开 >>e to Insufficient Efficacy) 收起 << | - | - |
NCT02737072 | Solid Tumor | Phase 1 | Terminated | - | - |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
0.84mL 0.17mL 0.08mL |
4.20mL 0.84mL 0.42mL |
8.41mL 1.68mL 0.84mL |
CAS号 | 1088715-84-7 |
分子式 | C62H88N14O10 |
分子量 | 1189.45 |
SMILES Code | O=C(NCC(N[C@@H](C(N[C@H](C(N)=O)CCCCNC(C)C)=O)CCC1=O)=O)[C@@H](NC([C@@]([H])(CCCNC(N)=N)NC([C@H](CCCCNC(C)C)NC([C@]([H])(CC2=CC=C(O)C=C2)NC([C@H](CC3=CC=CC=C3)N1)=O)=O)=O)=O)CC4=CC5=C(C=C4)C=CC=C5 |
MDL No. | MFCD30537218 |
别名 | |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C |
溶解方案 |
请根据您的动物给药指南选择适当的溶解方案。 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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