盐酸帕唑帕尼|T6930|TargetMol

Pazopanib Hydrochloride
635702-64-6

￥424 10mg 起订

￥931 50mg 起订

￥1339 100mg 起订

上海更新日期：2024-09-24

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：: 盐酸帕唑帕尼

英文名称：: Pazopanib Hydrochloride

CAS号：: 635702-64-6

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：: 99.69%

产品类别：: 抑制剂

货号：: T6930

Product Introduction

Bioactivity

名称	Pazopanib Hydrochloride
描述	Pazopanib Hydrochloride (Votrient HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively.
细胞实验	Phosphorylation of VEGFR2 is assessed in HUVEC stimulated with VEGF. HUVEC are plated in type-I collagen-coated 10 cm plates in Clonetics EGM-MV medium at 1.0-1.5 × 106 cells/plate. After 24 hours, the confluent cells are serum starved overnight by replacing the growth medium with Clonetics EBM medium containing 0.1% BSA, 500 μg/mL hydrocortisone. Cells are treated with Pazopanib at various concentrations for 1 hour, followed by addition of 10 ng/mL VEGF or vehicle for 10 min. Cells are solubilized in lysis buffer. VEGFR2 is immunoprecipitated using antiflk-1 antibody and analyzed by sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE) followed by Western blotting and detection with antiflk-1 or with antiphosphotyrosine (anti-P-tyr-biotin) antibody. The VEGFR2 phosphorylation level is quantified by densitometry and normalized to the total VEGFR2 level. (Only for Reference)
激酶实验	Kinase enzyme assays: 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 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 Pazopanib 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.
体外活性	Pazopanib以8 nM的IC50强效抑制VEGF诱导的VEGFR2在HUVEC细胞中的磷酸化。[1] Pazopanib对包括SYO-1和HS-SY-II细胞在内的所有滑膜肉瘤细胞系显示出剂量依赖性的生长抑制。即使在Pazopanib浓度为1μg/mL时，SYO-1和HS-SY-II细胞的增殖也受到抑制，并且在5μg/mL时完全停止。Pazopanib引发G1阶段停滞，从而抑制滑膜肉瘤细胞的生长。与对照组相比，Pazopanib处理的SYO-1细胞中Akts、GSK-3β、JNKs、p70 S6 Kinase和mTOR的磷酸化受到抑制。[2] 当Pazopanib浓度在20μg/mL到22.5μg/mL之间时，RPE细胞存活率呈现增加的减少。[3]
体内活性	经30mg/kg或100mg/kg Pazopanib处理的小鼠与接受安慰剂或10mg/kg Pazopanib处理的小鼠相比，肿瘤负担显著减少。Pazopanib的治疗具有良好的耐受性，各组小鼠之间的体重无显著差异。[2]
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) Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 7.5 mg/mL (15.82 mM), Sonication is recommended.
关键字	inhibit \| CD117 \| CSF1R \| Vascular endothelial growth factor receptor \| colony stimulating factor 1 receptor \| FGFR \| VEGFR \| Platelet-derived growth factor receptor \| GW 786034 \| CSF-1R \| SCFR \| GW-786034 \| Inhibitor \| Pazopanib Hydrochloride \| Autophagy \| Pazopanib \| c-Fms \| PDGFR \| c-Kit \| Fibroblast growth factor receptor \| CSF-1 receptor
相关产品	Guanidine hydrochloride \| Naringin \| Valproic Acid \| Taurine \| Gefitinib \| Aceglutamide \| Hydroxychloroquine \| Ferulic Acid \| Curcumin \| Stavudine \| Paeonol \| Sodium 4-phenylbutyrate
相关库	经典已知活性库 \| 抗癌活性化合物库 \| 抗癌上市药物库 \| 激酶抑制剂库 \| 抗衰老化合物库 \| FDA 上市药物库 \| 抗癌临床化合物库 \| 抗癌药物库

盐酸帕唑帕尼|||Votrient HCl|||Pazopanib HCl|||GW786034 HCl|||GW786034|||Armala|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