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  • 化合物 GW 2580|T2659|TargetMol

化合物 GW 2580|T2659|TargetMol

GW2580
870483-87-7
￥192 1mg 起订
￥387 5mg 起订
￥622 10mg 起订
上海 更新日期：2024-12-02

TargetMol中国（陶术生物）

VIP12年
联系人：邵小姐
电话：021-021-33632979拨打
手机：15002134094 拨打
邮箱：marketing@targetmol.com

产品详情:

中文名称：
化合物 GW 2580
英文名称：
GW2580
CAS号：
870483-87-7
品牌：
TargetMol
产地：
美国
保存条件：
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格：
99.86%
产品类别：
抑制剂
货号：
T2659

Product Introduction

Bioactivity

名称GW2580
描述GW2580 (SC-203877) is a specific, oral-bioavailable CSF-1R inhibitor for c-FMS.
细胞实验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)
激酶实验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.
体外活性在佐剂性关节炎模型中,GW2580（50 mg/kg ）能够抑制关节结缔组织和骨破坏.在小鼠中,口服 GW2580（40 mg/kg）能够抑制外源性CSF-1促进脂多糖诱导的TNF-α生成的能力.在腹腔内CSF-1依赖性的M-NFS-60肿瘤细胞模型中,口服 GW2580（80 mg/kg）能够抑制肿瘤细胞生长.在移植3LL肺肿瘤模型中,GW2580（160 mg/kg）能够抑制骨髓细胞的生长.
体内活性GW2580能够抑制多种细胞的生长,对于CSF-1刺激的M-NFS-60骨髓瘤细胞（IC50=0.33 μM）,血清刺激的NSO骨髓瘤细胞（IC50=13.5 μM）,CSF-1刺激的新鲜分离的人单核细胞（IC50=0.47 μM）,和血管内皮生长因子刺激的人脐静脉血管内皮细胞（IC50=12 μM）。对于TRKA（IC50=0.88 μM）,人类CFMS激酶（0.06 μM）GW2580能够发挥抑制作用。在RAW264.7小鼠巨噬细胞中（IC50=10 nM）,GW2580能通过抑制CSF1R磷酸化发挥作用。
存储条件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)
关键字c-Fms | GW2580 | SC203877 | inhibit | SC 203877 | GW-2580 | CSF1R | CSF-1 receptor | Inhibitor | CSF-1R | colony stimulating factor 1 receptor
相关产品Onatasertib | Cerdulatinib hydrochloride | Sotuletinib | PLX647 | Masitinib | c-Fms-IN-1 | Linifanib | c-Fms-IN-13 | Pexidartinib | PLX5622 | c-Fms-IN-3 | Pazopanib Hydrochloride
相关库抑制剂库 | 经典已知活性库 | 已知活性化合物库 | 激酶抑制剂库 | 高选择性抑制剂库 | NO PAINS 化合物库 | 干细胞分化化合物库 | 膜蛋白靶向化合物库 | 口服活性化合物库 | 酪氨酸激酶分子库
SC-203877|||GW 2580|TargetMol

公司简介

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。 从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。 经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期 (12年)
注册资本 566.2651万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,试剂,定制,服务
主营行业 化学试剂,生物活性小分子

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