GW2580
CFMS激酶/CSF-1R抑制剂
| 规格 | 价格 | 货期 | 数量 |
|---|---|---|---|
| 10mg | ￥590.00 | 现货 | |
| 50mg | ￥681.00 | 现货 | |
| 100mg | ￥863.00 | 现货 |
特色产品
- 适用于流式细胞仪和荧光显微镜检测
- 准确区分活细胞/凋亡细胞/坏死细胞
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白
- 对细胞无毒性
- 步骤更简单，无需有机溶剂
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
- 优异的扩增效率、可重复性和稳定性
- 卓越的灵敏度和准确性，操作简单
- 优化的缓冲液和T7 RNA聚合酶混合物
- 20 μL反应体系可获得更高的RNA产量
产品描述
GW2580是有选择性和口服生物利用度的集落刺激因子1受体（CSF-1R）抑制剂，IC50值为30 nM[1]。
GW2580被证明是一种极具选择性的CSF-1R抑制剂，猜测可与CSF-1R的DFG-out模式结合，使之处于无活性的构象[2]。GW2580可抑制上皮细胞相关的CSF-1信号，减少Gr-1+ CD11b+髓源抑制细胞（MDSCs）扩张，缓解免疫抑制微环境[3]。此外，GW2580在人类胶质母细胞瘤细胞系T98G中可抑制IL-10分泌[4]。
参考文献：
[1] Conway JG1, McDonald B, Parham J, Keith B, Rusnak DW, Shaw E, Jansen M, Lin P, Payne A, Crosby RM, Johnson JH, Frick L, Lin MH, Depee S, Tadepalli S,Votta B, James I, Fuller K, Chambers TJ, Kull FC, Chamberlain SD, Hutchins JT. Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580. Proc Natl Acad Sci U S A. 2005 Nov 1;102(44):16078-83.
[2] Garcia AJ1, Ruscetti M, Arenzana TL, Tran LM, Bianci-Frias D, Sybert E, Priceman SJ, Wu L, Nelson PS, Smale ST, Wu H. Pten Null Prostate Epithelium Promotes Localized Myeloid-Derived Suppressor Cell Expansion and Immune Suppression during Tumor Initiation and Progression. Mol Cell Biol. 2014 Jun;34(11):2017-28.
[3] Kitagawa D1, Gouda M, Kirii Y, Sugiyama N, Ishihama Y, Fujii I, Narumi Y, Akita K, Yokota K. Characterization of kinase inhibitors using different phosphorylation states of colony stimulating factor-1 receptor tyrosine kinase. J Biochem. 2012 Jan;151(1):47-55.
[4] Komohara Y1, Horlad H, Ohnishi K, Fujiwara Y, Bai B, Nakagawa T, Suzu S, Nakamura H, Kuratsu J, Takeya M. Importance of direct macrophage-tumor cell interaction on progression of human glioma. Cancer Sci. 2012 Dec;103(12):2165-72.
产品性质
| 物理外观 | Solid |
| CAS号 | 870483-87-7 |
| 分子式 | C20H22N4O3 |
| 分子量 | 366.41 |
| 化学名称 | 5-[[3-methoxy-4-[(4-methoxyphenyl)methoxy]phenyl]methyl]pyrimidine-2,4-diamine |
| 溶解度 | ≥36.6 mg/mL in DMSO with gentle warming; insoluble in EtOH; insoluble in H2O |
| SMILES | COc1ccc(COc(ccc(Cc2c(N)nc(N)nc2)c2)c2OC)cc1 |
| 存储条件 | -20°C |
| 运输条件 | 蓝冰 |
产品应用 (实验数据来自文献，APExBIO并未验证，仅供参考)
IC50和靶点
| 生物活性描述 | GW2580是选择性的cFMS激酶抑制剂；IC50值为0.03 μM。 | |
| 靶点 | cFMS kinase | CSF-1-induced monocyte growth |
| 生物活性数据 | 0.03 μM | 0.14 μM |
生物相关数据
APExBIO 顾客使用本产品发表的 5 篇科研文献
- 1. Bo Liu, Dongze Zhang, et al. "Red blood cell membrane-camouflaged poly (lactic-co-glycolic acid) microparticles as a potential controlled release drug delivery system for local stellate ganglion microinjection." Acta Biomater. 2023 Apr 15:161:201-212. PMID: 36858164
- 2. Jiqing Tang, Jun Liu, et al. "Konjac Glucomannan Oligosaccharides Prevent Intestinal Inflammation Through SIGNR1‐Mediated Regulation of Alternatively Activated Macrophages." Mol Nutr Food Res. 2021 Oct;65(20):e2001010. PMID:34390195
- 3. Ramadurgum P, Woodard DR, et al. "Simultaneous Control of Endogenous and User-Defined Genetic Pathways Using Unique ecDHFR Pharmacological Chaperones." Cell Chem Biol. 2020;27(5):622-634.e6. PMID:32330442
- 4. Alexandria N. Hughes, Bruce Appel. "Microglia phagocytose myelin sheaths to modify developmental myelination." Nature Neuroscience (2020); 06 July 2020.
- 5. Green LA, Nebiolo JC, et al. "Microglia exit the CNS in spinal root avulsion." PLoS Biol. 2019 Feb 22;17(2):e3000159. PMID:3000159
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