1. Protein Tyrosine Kinase/RTK Autophagy
  2. VEGFR c-Kit PDGFR Autophagy FGFR
  3. Pazopanib

Pazopanib  (Synonyms: 帕唑帕尼; GW786034)

目录号: HY-10208 纯度: 99.91%
COA 产品使用指南

Pazopanib (GW786034) 是多靶点抑制剂,抑制 VEGFR1VEGFR2VEGFR3PDGFRβc-KitFGFR1c-FmsIC50分别为10,30,47,84,74,140,146 nM。

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Pazopanib Chemical Structure

Pazopanib Chemical Structure

CAS No. : 444731-52-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥517
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1 mg ¥146
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5 mg ¥293
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10 mg ¥470
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50 mg ¥940
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100 mg ¥1380
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200 mg ¥2270
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500 mg ¥4500
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Top Publications Citing Use of Products

    Pazopanib purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2016;38(3):926-38.  [Abstract]

    Arithmetic means±SEM (n=16) of erythrocyte annexin-V-binding following incubation for 48 hours to Ringer solution without (white bar) or with (black bars) Pazopanib (10-50 µg/mL).

    查看 VEGFR 亚型特异性产品:

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    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.

    IC50 & Target[1]

    VEGFR1

    10 nM (IC50)

    VEGFR2

    30 nM (IC50)

    VEGFR3

    47 nM (IC50)

    PDGFRβ

    84 nM (IC50)

    FGFR1

    140 nM (IC50)

    c-Kit

    74 nM (IC50)

    c-Fms

    146 nM (IC50)

    体外研究
    (In Vitro)

    Pazopanib 显示出对所有人类 VEGFR 受体的良好效力,对 VEGFR-1、-2 和-3 的 IC50 分别为 10、30 和 47 nM。还观察到对密切相关的酪氨酸受体激酶 PDGFRβ、c-Kit、FGF-R1 和 c-fms 的显著活性,IC50 分别为 84、74、140 和 146 nM。在细胞试验中,除了抑制 VEGF 诱导的 HUVEC 增殖外,Pazopanib 还有效抑制 VEGF 诱导的 HUVEC 细胞中 VEGFR-2 的磷酸化,IC50 约为 8 nM。Pazopanib 在大鼠、狗和猴子中具有良好的药代动力学,分别在 10、1 和 5 mg/kg 时具有低清除率 (1.4-1.7 mL/min/kg) 和良好的口服生物利用度 (72%、47%、65%)。除了 2C9 (7.9 μM) 外,细胞色素 P450 谱也得到改善,对测试的同工酶的抑制 >10 μM[1]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    用 100 mg/kg 的 Pazopanib 处理小鼠,每天两次,持续 5 天,导致血管形成程度的显著抑制。使用 HT29 (结肠癌)、A375P (黑色素瘤) 和 HN5 (头颈癌) 肿瘤后,在携带已建立的人异种移植物 (200 250 mm3) 的小鼠中检查 Pazopanib 的抗血管生成活性标准的三周疗程。与 A375P 模型相比,HN5 和 HT29 异种移植物在所有剂量下的反应都更好,A375P 模型历来对 VEGFR-2 抑制剂具有更强的耐药性。作为支持观察到的异种移植物生长抑制是通过抗血管生成而非抗肿瘤机制发挥作用的证据,在低于 10 μM 的浓度下未观察到 Pazopanib 对这些在含血清培养基中生长的人类肿瘤细胞系 (HT29、HN5、A375P) 的抗增殖活性。未观察到对小鼠体重的显著影响,并且在整个研究期间动物看起来健康且活跃[1]
    Pazopanib 滴眼液组粘附的白细胞数量低于未处理的糖尿病动物,高于健康动物。粘附在健康动物视网膜脉管系统上的平均白细胞为 37.2±7.8,而糖尿病动物的平均值为 102±15.6,比健康动物高约 3 倍。用 0.5 % w/v Pazopanib 混悬液处理的动物在其视网膜血管系统中粘附了 69.5±9.5 个白细胞,这明显低于糖尿病动物[2]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    分子量

    437.52

    Formula

    C21H23N7O2S

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    帕唑帕尼

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 50 mg/mL (114.28 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.2856 mL 11.4280 mL 22.8561 mL
    5 mM 0.4571 mL 2.2856 mL 4.5712 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.71 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.71 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.91%

    参考文献
    Kinase Assay
    [1]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1][2]

    Mice[1]
    Tumors are initiated by injection of tumor cell suspension in 8−12 week old nude mice. When tumors reach a volume of 100−200 mm3, mice are randomized and divided into groups of eight. Pazopanib is administered once or twice daily at 10, 30, or 100 mg/kg. Animals are euthanized by inhalation of CO2 at the completion of the study. Tumor volume is measured twice weekly by calipers, using the equation: tumor volume (mm3)=(length×width2)/2. Results are routinely reported as % inhibition=1−(average growth of the drug treated population/average growth of vehicle treated control population).
    Rats[2]
    Male Brown-Norway (BN; pigmented) rats weighing 200 to 250 g are acclimatized for at least two days prior to any experimental procedure. After overnight fasting for 12-16 h, an intraperitoneal injection of 30 mg/mL solution of Streptozotocin in 10 mM citrate buffer (pH 4.5) is administered (60 mg/kg body weight) to induce diabetes. After 3-4 h of Streptozotocin injection, animals are put on a regular diet and 24 h after Streptozotocin injection, blood sample (5-10 μL) is collected via tail vein. The blood glucose levels in the animals are determined with a glucose monitor. Animals with blood glucose levels greater than 250 mg/dL are considered diabetic. The animals are divided into three groups. Group 1: Healthy (n=12), Group 2: Diabetic (n=12) and Group 3: Diabetic+Treatment (n=12). Treatment is started immediately after diabetes induction. Both eyes are dosed twice daily for 30 days with 0.5 % w/v Pazopanib suspension (10 μL volume in each eye) and animals in all groups are sacrificed on day 31, 16-17 h after last dose on day 30.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2856 mL 11.4280 mL 22.8561 mL 57.1402 mL
    5 mM 0.4571 mL 2.2856 mL 4.5712 mL 11.4280 mL
    10 mM 0.2286 mL 1.1428 mL 2.2856 mL 5.7140 mL
    15 mM 0.1524 mL 0.7619 mL 1.5237 mL 3.8093 mL
    20 mM 0.1143 mL 0.5714 mL 1.1428 mL 2.8570 mL
    25 mM 0.0914 mL 0.4571 mL 0.9142 mL 2.2856 mL
    30 mM 0.0762 mL 0.3809 mL 0.7619 mL 1.9047 mL
    40 mM 0.0571 mL 0.2857 mL 0.5714 mL 1.4285 mL
    50 mM 0.0457 mL 0.2286 mL 0.4571 mL 1.1428 mL
    60 mM 0.0381 mL 0.1905 mL 0.3809 mL 0.9523 mL
    80 mM 0.0286 mL 0.1429 mL 0.2857 mL 0.7143 mL
    100 mM 0.0229 mL 0.1143 mL 0.2286 mL 0.5714 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    产品名称:
    Pazopanib
    目录号:
    HY-10208
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