| GW2580CFMS kinase/CSF-1R inhibitor,selective and ATP-competitive |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
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- Purity = 99.76%
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- NMR (Nuclear Magnetic Resonance)
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- Datasheet
Chemical structure
Related Biological Data
| Description | GW2580 is a selective inhibitor of cFMS kinase with IC50 value of 0.03 μM. | |||||
| Targets | cFMS kinase | CSF-1-induced monocyte growth | ||||
| IC50 | 0.03 μM | 0.14 μM | ||||
| Cell experiment [1]: | |
Cell lines | Mouse M-NFS-60 myeloid cell line and human monocytes |
Preparation method | The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | 0- 20 μM |
Applications | GW2580 at 1 μM completely inhibited CSF-1-induced growth of mouse M-NFS-60 myeloid cells and human monocytes and completely inhibited bone degradation in cultures of human osteoclasts, rat calvaria, and rat fetal long bone. In contrast, GW2580 did not affect the growth of mouse NS0 lymphoblastoid cells, human endothelial cells, human fibroblasts, or five human tumor cell lines. |
| Animal experiment [1]: | |
Animal models | Xenograft mouse model with M-NFS-60 tumor cells |
Dosage form | Orally at 20 and 80 mg/kg twice a day |
Application | GW2580 was dosed orally at 20 and 80 mg/kg (b.i.d.), starting 1 h before the i.p. injection of M-NFS-60 cells, and the tumor cells in the peritoneal cavity were counted 4 days later. GW2580 produced a dose-related decrease in the number of tumor cells, with the 80 mg/kg dose completely blocking tumor growth. GW2580 showed no effect on body weights taken when the animals were killed. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [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. | |
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| Cas No. | 870483-87-7 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | 5-[[3-methoxy-4-[(4-methoxyphenyl)methoxy]phenyl]methyl]pyrimidine-2,4-diamine | ||
| Canonical SMILES | COC1=CC=C(C=C1)COC2=C(C=C(C=C2)CC3=CN=C(N=C3N)N)OC | ||
| Formula | C20H22N4O3 | M.Wt | 366.41 |
| Solubility | ≥36.6mg/mL in DMSO with gentle warming | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
GW2580 is a selective and orally bioavailable inhibitor of Colony-stimulating-factor-1 receptor (CSF-1R) with IC50 value of 30nM [1]
GW2580 has been demonstrated to be an extremely selective inhibitor for CSF-1R and has been hypothesized to bind to the DFG-out mode of CSF-1R, which might lock it into an inactive conformation [2] GW2580 has shown to inhibit epithelial cell-associated CSF-1 signaling, reduce Gr-1+ CD11b+ myeloid-derived suppressor cells (MDSCs) expansion, and alleviate the immune-suppressive microenvironment [3]. In addition, GW2580 suppressed IL-10 secretion in human glioblastoma cell line T98G [4].
References:[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.
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为了使供输血用的血液能保存一定时间，加入适当的抗凝剂，并尽量防止在保存期发生变质而用的液体。为了防止因糖的消失引起活力降低，尚加入葡萄糖。ACD液（含柠檬酸三钠、柠檬酸、葡萄糖）一般用于血库。添加ACD的血液放在4—6℃条件下保存，可保存三周。另外为防止柠檬酸盐的过量可用加磷酸钠的CPD液。此外还设计了加乳酸钠的ACDL液。如果加入甘油等防冻剂则可长时间冷冻保存红细胞。
我搜索了一下网络上的，只找到说要保存在酸性下，但是没有具体的配方。
目前选择这个都是北京博凌科为生物科技有限公司的
小白一枚，现在要构建紫杉醇细胞耐药株。但是我们实验室紫杉醇是医用注射液，浓度为6mg/ml。这个浓度太大了，工作液浓度都是几十ng/ml。想问一下各位大神该如何配置成浓度相对低一点的储存液呢，有效期可以有多久呢？
目前正在从新鲜病人肿瘤组织标本中提取细胞悬液进行阳性细胞的筛选，但由于实验室距离医院有3个小时的车程，请问什么储存方法或者储存液能短期保证肿瘤组织中细胞完整性？谢谢
