XRK3F2
产品说明书
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同义名 : | - |
| CAS号 : | 2375193-43-2 | |
| 货号 : | A878726 | |
| 分子式 : | C23H24ClF2NO3 | |
| 纯度 : | 99%+ | |
| 分子量 : | 435.891 | |
| MDL号 : | MFCD31812777 | |
| 存储条件： |
Pure form Inert atmosphere,Room Temperature In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 145 mg/mL(332.65 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | p62 (sequestosome 1) serves as a signaling hub in BMSC (bone marrow stromal cells) for the formation of signaling complexes involved in the BMSC-induced increase in osteoclastogenesis and MM cell growth characteristic of MMBD, including NFκB, p38MAPK, and JNK, and the ZZ-domain of p62 (p62-ZZ) is required for BMSC enhancement of MMBD[1]. XRK3F2, a novel small molecule inhibitor the p62-ZZ domain of signaling, which blocks TNFα and MM activation of downstream signaling from the p62-signaling hubblunted MM (Multiple myeloma)-induced Runx2 suppression in vitro, and induced new bone formation and remodeling in the presence of tumor in vivo. In addition, XRK3F2 also directly decreased osteoclast (OCL) formation. Further, XRK3F2 directly inhibited cell growth of primary CD138+ MM cells and human MM cell lines in vitro, without negatively affecting the growth of BMSC[2]. In a vitro dtudy, primary MM cells, human MM cell lines, or murine 5TGM1-gfp cells were incubated with XRK3F2 for 48h or 72h in concentrations of 10 mg/ml for 0 – 30 mins. It demonstrated that XRK3F2 blocks TNFα-induced signaling processes in MM patient BMSC and MM cells. The IC50 of XRK3F2 for 5TGM1 cells was 4.35 µM, and 4.6 µM for the human MM1.S cell line. 1 × 105 5TGM1-gfp cells in logarithmic phase growth were inoculated into one tibia (IT) of C57BL/KaLwRij mice and the mice were treated with either XRK3F2 (27 mg/kg/day or 40 mg/kg/day) or vehicle. Six of 17 XRK3F2-treated and 1 vehicle-treated animal demonstrated a marked periosteal reaction on x-ray, suggesting new bone formation along the tibia, which showed that XRK3F2 induced dramatic, local new bone formation in bones bearing MM in vivo[2]. | ||
| 作用机制 | XRK3F2 selective blocking of the p62-ZZ domain-signaling module, may also influence cytoplasmicnuclear shuttling and/or Ajuba-dependent binding of GFI1 to the Runx2 promoter[1]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.29mL 0.46mL 0.23mL |
11.47mL 2.29mL 1.15mL |
22.94mL 4.59mL 2.29mL |
| 参考文献 |
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