GW2580 NEW
| Price | $43 | $63 | $79 |
| Package | 5mg | 10mg | 50mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-14 |
Product Details
| Product Name: GW2580 | CAS No.: 870483-87-7 |
| Purity: 99.86% | Supply Ability: 10g |
| Release date: 2024/11/14 |
Product Introduction
Bioactivity
| 名稱 | GW2580 |
| 描述 | GW2580 (SC-203877) is a specific, oral-bioavailable CSF-1R inhibitor for c-FMS. |
| 細(xì)胞實(shí)驗(yàn) | One day before the start of the cell growth assay the cells are spun down and placed in a depleted media at 2× 106 cells per ml for 24 h. Depleted medium for M-NSF60 cells lacks MCSF. The next day, GW2580 at 10 mM in DMSO is diluted to 20 μM and 0.2% DMSO in medium containing 10% serum and serially diluted to yield a 10-point concentration curve. The M-NFS-60 cells are resuspended in medium at 0.5× 106 cells/mL with 10% serum and 20 ng/mL mouse MCSF. Cells (50 μL) are added to each well containing inhibitor (50 μL), and, 3 days later, 10 μL of WST-1 reagent is added to each well. After a 4-h incubation, the absorbance is measured at 440 nm and growth calculated as the difference between wells with full medium and wells with depleted medium.(Only for Reference) |
| 激酶實(shí)驗(yàn) | cFMS tyrosine kinase assay: The enzyme is activated by autophosphorylation by incubating 10 μM enzyme, 100 μM ATP, and 5 mM MgCl2 in 50 mM Tris HCL for 90 min at room temperature. Enzyme reactions are performed in a volume of 45 μL, by using round-bottom polystyrene 96-well plates on a Biomek 2000. Compound in 1 μL DMSO or DMSO alone are added to each well containing 30 μL of a 1.5× substrate reaction mix containing 50 mM Mops (3-[N-Morpholino]propanesulfonic acid), pH 7.5, 15 mM MgCl2, 6 μM peptide substrate, biotin-EAIYAPFAKKK-NH2 7.5 mM DTT, 75 mM NaCl, 10 μM ATP, and 0.5 μCi (1 Ci = 37 GBq) [33P-γ] ATP per assay. The reaction is initiated by the addition of 15 μL of diluted enzyme solution, resulting in a final enzyme concentration 20 nM. EDTA is added to control wells for determination of background. The reaction is allowed to proceed for 40 min and stopped by the addition of an equal volume of 0.5% phosphoric acid, and 75 μL is transferred to a 96-well phosphocellulose filter plate that has been prewet with 100 μL of 0.5% phosphoric acid. The plate is filtered on a Millipore filter-plate vacuum manifold and washed three times with the phosphoric acid solution, followed by the addition of 40 μL of scintillation solution. The plates are sealed and counted in a Packard Topcount NXT scintillation counter. |
| 體外活性 | In adjuvant-induced arthritis models, GW2580 (50 mg/kg) effectively inhibits the destruction of joint connective tissue and bone. In mice, the oral administration of GW2580 (40 mg/kg) suppresses the ability of exogenous CSF-1 to enhance lipopolysaccharide-induced TNF-α production. Furthermore, in an intraperitoneal CSF-1 dependent M-NFS-60 tumor cell model, oral GW2580 (80 mg/kg) inhibits tumor cell growth. In transplantable 3LL lung tumor models, GW2580 (160 mg/kg) effectively restricts the growth of bone marrow cells. |
| 體內(nèi)活性 | GW2580 effectively inhibits growth in various cell types, demonstrating activity against M-NFS-60 myeloma cells stimulated by CSF-1 (IC50=0.33 μM), NSO myeloma cells stimulated by serum (IC50=13.5 μM), freshly isolated human monocytes stimulated by CSF-1 (IC50=0.47 μM), and human umbilical vein endothelial cells stimulated by vascular endothelial growth factor (IC50=12 μM). It also exhibits inhibitory effects on TRKA (IC50=0.88 μM) and human CFMS kinase (0.06 μM). In RAW264.7 mouse macrophages (IC50=10 nM), GW2580 operates by inhibiting the phosphorylation of CSF1R. |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 15 mg/mL (40.94 mM) Ethanol : < 1 mg/mL (insoluble or slightly soluble) |
| 關(guān)鍵字 | c-Fms | GW2580 | SC203877 | inhibit | SC 203877 | GW-2580 | CSF1R | CSF-1 receptor | Inhibitor | CSF-1R | colony stimulating factor 1 receptor |
| 相關(guān)產(chǎn)品 | c-Fms-IN-3 | PLX5622 | c-Fms-IN-1 | Sotuletinib | Ki20227 | Pazopanib Hydrochloride | Pexidartinib | c-Fms-IN-13 | Linifanib | Masitinib | Cerdulatinib hydrochloride | Onatasertib |
| 相關(guān)庫 | 高選擇性抑制劑庫 | 經(jīng)典已知活性庫 | 膜蛋白靶向化合物庫 | 激酶抑制劑庫 | 酪氨酸激酶分子庫 | 抑制劑庫 | 干細(xì)胞分化化合物庫 | NO PAINS 化合物庫 | 口服活性化合物庫 | 已知活性化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Anhui Ruihan Technology Co., Ltd
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2023-08-21 |
United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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