帕唑帕尼|T0097L

Pazopanib
444731-52-6

￥292 10mg 起订

￥472 25mg 起订

￥783 50mg 起订

上海更新日期：2024-09-14

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：: 帕唑帕尼

英文名称：: Pazopanib

CAS号：: 444731-52-6

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：: 99.84%

产品类别：: 抑制剂

货号：: T0097L

Product Introduction

Bioactivity

名称	Pazopanib
描述	Pazopanib (GW786034) is an inhibitor of protein tyrosine kinases that inhibits VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms (IC50=10/30/47/84/74/140/146 nM). Pazopanib has antitumor activity.
细胞实验	Pazopanib is prepared in DMSO and then diluted to final concentration in medium[1]. The effect of Pazopanib on cell proliferation is measured using 5-bromo-2-deoxyuridine (BrdU) incorporation method using commercially available kits. HUVEC is seeded in medium containing 5% fetal bovine serum (FBS) in type 1 collagen coated 96-well plates and incubated overnight at 37°C, 5% CO2. The medium is aspirated from the cells, and various concentrations of Pazopanib in serum-free medium are added to each well. After 30 min, either VEGF (10 ng/mL) or bFGF (0.3 ng/mL) is added to the wells. Cells are incubated for an additional 72 h and BrdU (10 μM) is added during the last 18 to 24 h of incubation. At the end of incubation, BrdU incorporation in cells is measured by ELISA. Data are fitted with a curve described by the equation, y=Vmax(1?(x/(K+x))), where K is equal to the IC50[1].
激酶实验	VEGFR enzyme assays for VEGGR1, VEGFR2, and VEGFR3 are run in homogeneous time-resolved fluorescence (HTRF) format in 384-well microtiter plates using a purified, baculovirus-expressed glutathione-S-transferase (GST) fusion protein encoding the catalytic c-terminus of human VEGFR receptor kinases 1, 2, or 3. Reactions are initiated by the addition of 10 μL of activated VEGFR2 kinase solution [final concentration, 1 nM enzyme in 0.1 M 4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES), pH 7.5, containing 0.1 mg/mL bovine serum albumin (BSA), 300 μM dithiothreitol (DTT)] to 10 μL substrate solution [final concentration, 360 nM peptide, (biotin-aminohexyl-EEEEYFELVAKKKK-NH2), 75 μM ATP, 10 μM MgCl2], and 1 μL of titrated compound in DMSO. Plates are incubated at room temperature for 60 min, and then the reaction is quenched by the addition of 20 μL of 100 mM ethylene diamine tetraacetic acid (EDTA). After quenching, 20 μL HTRF reagents (final concentration, 15 nM Streptavidin-linked allophycocyanin, 1 nM Europium-labeled antiphosphotyrosine antibody diluted in 0.1 mg/mL BSA, 0.1 M HEPES, pH 7.5) is added and the plates incubated for a minimum of 10 min. The fluorescence at 665 nM is measured with a Wallac Victor plate reader using a time delay of 50 μs[1].
体外活性	方法: SCLC 细胞系 NCI-H446 和 NCI-H82 用 Pazopanib (0.01-30 µM) 处理 24-72 h，通过 CCK-8 assay 检测细胞活力。结果: Pazopanib 以剂量和时间依赖的方式显著降低了 NCI-H446 细胞的增殖，24 h 时 IC50 值为 1.05 µM。Pazopanib 还可以以剂量和时间依赖的方式诱导 NCI-H82 细胞中的强效细胞死亡，24 h 的 IC50 为 1.298 µM。Pazopanib 显著拮抗小细胞肺癌细胞增殖。[1] 方法: 人结直肠癌细胞 HCT-116 用 Pazopanib (1-20 µM) 处理 3-24 h，通过 Western Blot 检测靶点蛋白表达水平。结果: Pazopanib 显著诱导了 PUMA 的表达，这是时间和剂量依赖性的。[2]
体内活性	方法: 为检测体内抗肿瘤活性，将 Pazopanib (30 mg/kg，suspended in 0.5% hydroxypropylmethyl cellulose and 0.1% Tween-80 in water) 灌胃给药给携带 NCI-H446 异种移植物的 NOD-SCID 小鼠，每天一次，持续两周。结果: Pazopanib 的给药显著抑制了 NCI-H446 异种移植物的生长。[1]
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 20 mg/mL (45.71 mM)
关键字	FGFR \| Autophagy \| Platelet-derived growth factor receptor \| Pazopanib \| GW 786034 \| c-Kit \| PDGFR \| Vascular endothelial growth factor receptor \| CD117 \| inhibit \| VEGFR \| Fibroblast growth factor receptor \| GW-786034 \| Inhibitor \| SCFR
相关产品	Guanidine hydrochloride \| Naringin \| Taurine \| Gefitinib \| Hydroxychloroquine \| Ferulic Acid \| Curcumin \| Stavudine \| Paeonol \| Sodium 4-phenylbutyrate
相关库	抑制剂库 \| 抗癌活性化合物库 \| 抗癌上市药物库 \| 已知活性化合物库 \| EMA 上市药物库 \| 抗衰老化合物库 \| 膜蛋白靶向化合物库 \| 酪氨酸激酶分子库 \| 药物功能重定位化合物库 \| FDA 上市激酶抑制剂库

帕唑帕尼|||GW786034|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