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  • 瓦他拉尼|T6720|TargetMol

瓦他拉尼|T6720|TargetMol

Vatalanib dihydrochloride
212141-51-0
￥113 1mg 起订
￥228 5mg 起订
￥372 10mg 起订
上海 更新日期：2024-12-12

TargetMol中国（陶术生物）

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联系人：邵小姐
手机：4008200310 拨打
邮箱：marketing@tsbiochem.com

产品详情:

中文名称：
瓦他拉尼
英文名称：
Vatalanib dihydrochloride
CAS号：
212141-51-0
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：
100%
产品类别：
抑制剂
货号：
T6720

Product Introduction

Bioactivity

名称Vatalanib dihydrochloride
描述Vatalanib dihydrochloride (PTK787 dihydrochloride)(IC50=37 nM) is an inhibitor of VEGFR2/KDR. It exhibits less effective against VEGFR1/Flt-1 and 18-fold against VEGFR3/Flt-4.
细胞实验As a test of the ability of PTK787/ZK 222584 to inhibit a functional response to VEGF, an endothelial cell proliferation assay, based on BrdUrd incorporation is used. Subconfluent HUVECs are seeded into 96-well plates coated with 1.5% gelatin and then incubated at 37 °C and 5% CO2 in growth medium. After 24 hours, growth medium is replaced by basal medium containing 1.5% FCS and a constant concentration of VEGF (50 ng/mL), bFGF (0.5 ng/mL), or FCS (5%), in the presence or absence of PTK787/ZK 222584. As a control, wells without growth factor are also included. After 24 hours of incubation, BrdUrd labeling solution is added, and cells incubated an additional 24 hours before fixation, blocking, and addition of peroxidase-labeled anti-BrdUrd antibody. Bound antibody is then detected using 3,3′5,5′-tetramethylbenzidine substrate, which results in a colored reaction product that is quantified spectrophotometrically at 450 nm. (Only for Reference)
激酶实验VEGF Receptor Tyrosine Kinase Assays : The in vitro kinase assays are performed in 96-well plates as a filter binding assay, using the recombinant GST-fused kinase domains expressed in baculovirus and purified over glutathione-Sepharose. γ-[33P]ATP is used as the phosphate donor, and poly-(Glu:Tyr 4:1) peptide is used as the acceptor. Recombinant GST-fusion proteins are diluted in 20 mM Tris·HCl (pH 7.5) containing 1–3 mM MnCl2, 3–10 mM MgCl2, 0.25 mg/mL polyethylene glycol 20000, and 1 mM DTT, according to their specific activity. Each GST-fused kinase is incubated under optimized buffer conditions [20 mM Tris-HCl buffer (pH 7.5), 1–3 mM MnCl2, 3–10 mM MgCl2, 3–8 μg/mL poly-(Glu:Tyr 4:1), 0.25 mg/mL polyethylene glycol 20000, 8 μM ATP, 10 μM sodium vanadate, 1 mM DTT, and 0.2 μCi[γ-33P]ATP in a total volume of 30 μL in the presence or absence of a test substance for 10 minutes at ambient temperature. The reaction is stopped by adding 10 μL of 250 mM EDTA. Using a 96-well filter system, half the volume (20 μL) is transferred onto a Immobilon-polyvinylidene difluoride membrane. The membrane is then washed extensively in 0.5% H3PO4 and then soaked in ethanol. After drying, Microscint cocktail is added, and scintillation counting is performed. IC50s for PTK787/ZK 222584 or SU5416 in these as well as all assays described below are calculated by linear regression analysis of the percentage inhibition.
体外活性Vatalanib对Flk、c-Kit和PDGFRβ的抑制作用分别表现在IC50为270 nM、730 nM和580 nM。此外，通过抑制VEGF在HUVECs中诱导的胸腺嘧啶核苷酸的结合，Vatalanib展现了IC50为7.1 nM的抗增殖效果，并且在相同的剂量范围内，剂量依赖性抑制VEGF诱导的内皮细胞的存活和迁移，而对不表达VEGF受体的细胞没有细胞毒性或抗增殖作用。[1] 最近的研究表明，Vatalanib显著抑制肝细胞性癌细胞的生长，并通过增加Bax蛋白水平和降低Bcl-xL与Bcl-2，增强了IFN/5-FU诱导的细胞凋亡。[2]
体内活性Vatalanib 通过每日一次口服（25-100 mg/kg）在生长因子植入模型和肿瘤细胞驱动的血管生成模型中对 VEGF 和 PDGF 的血管生成反应产生剂量依赖性抑制。在相同剂量范围内，Vatalanib 还能抑制裸鼠体内多种人类癌症的生长和转移，而对循环血细胞或骨髓白细胞无显著影响。[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DMSO : 79 mg/mL (188.2 mM)
H2O : 10 mg/mL (23.82 mM)
Ethanol : 6 mg/mL (14.29 mM)
关键字Inhibitor | Vascular endothelial growth factor receptor | CGP-79787 | VEGFR | CGP-797870 | Vatalanib | PTK787 Dihydrochloride | ZK222584 | PTK 787 Dihydrochloride | PTK-787 Dihydrochloride | Apoptosis | CGP797870 | PTK-787 | CGP 797870 Dihydrochloride | Vatalanib dihydrochloride | CGP79787 Dihydrochloride | ZK-222584 | ZK 222584 | ZK 222584 Dihydrochloride | CGP 79787 | ZK-222584 Dihydrochloride | PTK 787 | CGP 79787 Dihydrochloride | CGP797870 Dihydrochloride | CGP 797870 | CGP-797870 Dihydrochloride | ZK222584 Dihydrochloride | PTK787 | Vatalanib (PTK787) | inhibit | CGP-79787 Dihydrochloride | Vatalanib Dihydrochloride | CGP79787
相关产品L-Glutamic acid | Metronidazole | 5-Fluorouracil | Dextran sulfate sodium salt (MW 4500-5500) | Stavudine | Tributyrin | Myricetin | Sorafenib | L-Ascorbic acid | Acetylcysteine | Salicylic acid | Sodium 4-phenylbutyrate
相关库抑制剂库 | 抗癌活性化合物库 | 经典已知活性库 | 膜蛋白靶向化合物库 | 药物功能重定位化合物库 | 酪氨酸激酶分子库 | 抗癌临床化合物库 | 抗癌药物库
瓦他拉尼|||ZK-222584 dihydrochloride|||Vatalanib 2HCl|||Vatalanib (PTK787) 2HCl|||PTK787 dihydrochloride|||CGP-797870 dihydrochloride|||CGP-79787 dihydrochloride|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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