化合物 PD173074|T2642|TargetMol

PD173074
219580-11-7

￥196 1mg 起订

￥438 5mg 起订

￥653 10mg 起订

上海更新日期：2024-09-23

TargetMol中国（陶术生物）

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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 PD173074

英文名称：: PD173074

CAS号：: 219580-11-7

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：: 98.21%

产品类别：: 抑制剂

货号：: T2642

Product Introduction

Bioactivity

Name	PD173074
Description	PD173074 is an effective FGFR1 inhibitor (IC50: 25 nM) and also inhibits VEGFR2 (IC50: 100-200 nM) in cell-free assays. The selectivity is higher ~1000-fold for FGFR1 than PDGFR and c-Src.
Cell Research	Cells are incubated with increasing concentrations of PD173074 in the presence of aFGF/heparin for 48 hours. The percentage of viable cells is determined by MTT.(Only for Reference)
Kinase Assay	In vitro kinase inhibition assays: Assays using the full-length FGFR-1 kinase are performed in a total volume of 100 μL containing 25 mM HEPES buffer (pH 7.4), 150 mM NaCl, 10 mM MnCl2, 0.2 mM sodium orthovanadate, 750 μg/mL concentration of a random copolymer of glutamic acid and tyrosine (4:1), various concentrations of PD173074 and 60 to 75 ng of enzyme. The reaction is initiated by the addition of [γ-32P]ATP (5 μM ATP containing 0.4 μCi of [γ-32P]ATP per incubation), and samples are incubated at 25°C for 10 minutes. The reaction is terminated by the addition of 30% trichloroacetic acid and the precipitation of material onto glass-fiber filter mats. Filters are washed three times with 15% trichloroacetic acid, and the incorporation of [32P] into the glutamate tyrosine polymer substrate is determined by counting the radioactivity retained on the filters in a Wallac 1250 betaplate reader. Nonspecific activity is defined as radioactivity retained on the filters following incubation of samples without enzyme. Specific activity is determined as total activity (enzyme plus buffer) minus nonspecific activity. The concentration of PD173074 that inhibits FGFR-1 enzymatic activity by 50% (IC50) is determined graphically.
In vitro	在KMS11异种移植瘤模型中,PD173074抑制FGFR3造成的肿瘤生长延缓,提高小鼠存活率. 在H-510异种移植体中,PD173074与顺铂阻断肿瘤生长的作用相似,与对照组相比中位生存期增加.在H-69异种移植体中,PD173074对50％小鼠的诱导作用大于6个月.PD173074（1/2 mg/kg/day）剂量依赖性地有效阻止由成纤维生长因子或血管内皮生长因子诱导的小鼠血管生成,且无明显毒性.在裸鼠体内,PD173074对NIH 3T3细胞（成纤维细胞生长因子受体3突变体转染）生长有抑制作用.
In vivo	PD173074剂量依赖性地抑制VEGFR2（IC50：100-200 nM）和FGFR1（IC50：1-5 nM）的自身磷酸化。 PD173074剂量依赖性抑制FGF-2促进的颗粒神经元存活（IC50：12 nM）,比SU 5402活性高1,000倍以上。 PD173074对FGF-2-介导的少突胶质细胞谱系细胞的细胞增殖、分化及MAPK激活具有特异性的抑制作用。PD173074是ATP竞争性的FGFR1抑制剂（Ki：40 nM）。PD173074还剂量依赖性地有效抑制FGFR3的自磷酸化（IC50：5 nM）。在多发性骨髓瘤细胞系中,PD173074对野生型及FGFR3突变型有活性。PD173074使表达FGFR3的KMS11细胞和KMS18细胞的活力显著下降（IC50<20 nM）。
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	Ethanol : 52.4 mg/mL (100 mM) DMSO : 60 mg/mL (114.58 mM)
Keywords	Inhibitor \| PD173074 \| Fibroblast growth factor receptor \| Apoptosis \| PD 173074 \| Vascular endothelial growth factor receptor \| inhibit \| FGFR \| PD-173074 \| VEGFR
Inhibitors Related	Gefitinib \| Metronidazole \| Ferulic Acid \| 5-Fluorouracil \| Stavudine \| Tributyrin \| Dextran sulfate sodium salt (MW 4500-5500) \| Myricetin \| Sorafenib \| L-Ascorbic acid \| Acetylcysteine \| Sodium 4-phenylbutyrate
Related Compound Libraries	Inhibitor Library \| Anti-Cancer Active Compound Library \| Bioactive Compound Library \| Bioactive Compounds Library Max \| Kinase Inhibitor Library \| Anti-Fibrosis Compound Library \| Anti-Aging Compound Library \| Highly Selective Inhibitor Library \| Membrane Protein-targeted Compound Library \| Tyrosine Kinase Inhibitor Library

PD173074|TargetMol

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