推荐产品
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
FC(F)(F)Oc1ccc(cc1)CC(=O)N(Cc5cnccc5)C(=C2Nc3ncccc3C(=O)N2c4ccc(cc4)OCC)C
InChI
1S/C32H28F3N5O4/c1-3-43-25-14-10-24(11-15-25)40-30(38-29-27(31(40)42)7-5-17-37-29)21(2)39(20-23-6-4-16-36-19-23)28(41)18-22-8-12-26(13-9-22)44-32(33,34)35/h4-17,19H,3,18,20H2,1-2H3,(H,37,38)
InChI key
IEKPMGNVFDUVPK-UHFFFAOYSA-N
生化/生理作用
AMG 487 is an orally available, potent and selective chemokine (C-X-C motif) receptor 3 (CXCR3) antagonist (IC50 = 8/8.2 nM against CXCL10/11 (IP-10/ITAC) for CXCR3 binding) that inhibits CXCR3 ligands-induced cell migration (CXCL10/11/9 IC50 = 8/15/36 nM). AMG 487 inhibits ITAC-induced calcium mobilization in vitro (IC50 = 5 nM) and reduces bleomycin-induced cellular lung recruitment in wild-type mice to the same level as in Cxcr3-deficient mice in vivo (3 mg/kg b.i.d. s.c.).
Orally available, potent and selective chemokine (C-X-C motif) receptor 3 (CXCR3) antagonist in vitro and in vivo.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
历史批次信息供参考:
Tonya C Walser et al.
Cancer research, 66(15), 7701-7707 (2006-08-04)
Tumor cells aberrantly express chemokines and/or chemokine receptors, and some may promote tumor growth and metastasis. We examined the expression and function of chemokine receptor CXCR3 in a syngeneic murine model of metastatic breast cancer. By flow cytometry, CXCR3 was
CXCL9 secreted by tumor-associated dendritic cells up-regulates PD-L1 expression in bladder cancer cells by activating the CXCR3 signaling
BMC Immunology, 22(1), 3-3 (2021)
Michael Johnson et al.
Bioorganic & medicinal chemistry letters, 17(12), 3339-3343 (2007-04-24)
A series of quinazolinone-derived inhibitors of the CXCR3 receptor have been synthesized and their affinity for the receptor evaluated. Compounds were evaluated in a (125)I-IP10 displacement assay and in in vitro cell migration assays to IP10, ITAC, and MIG using
Ming-Xia Zhu et al.
Experimental cell research, 397(2), 112365-112365 (2020-11-17)
Mantle cell lymphoma (MCL) is a unique subtype of B-cell non-Hodgkin lymphoma with a generally aggressive and heterogeneous clinical course. Chemokines are one of the complex components in the tumor microenvironment (TME), and they play a vital role in tumor
Jin Qian et al.
Cell communication and signaling : CCS, 19(1), 9-9 (2021-01-23)
To investigate the effect of lactic acid (LA) on the progression of bone metastasis from colorectal cancer (CRC) and its regulatory effects on primary CD115 (+) osteoclast (OC) precursors. The BrdU assay, Annexin-V/PI assay, TRAP staining and immunofluorescence were performed
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