1. Protein Tyrosine Kinase/RTK
  2. c-Kit VEGFR
  3. Motesanib Diphosphate

Motesanib Diphosphate  (Synonyms: AMG 706 Diphosphate)

目录号: HY-10229 纯度: 99.64%
COA 产品使用指南

Motesanib Diphosphate (AMG 706 Diphosphate) 是一种有效的 VEGFR1/2/3 的 ATP 竞争性抑制剂,IC50 值为 2 nM/3 nM/6 nM,与对 Kit 的选择性相似,是 PDGFRRet 的 10 倍多。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Motesanib Diphosphate Chemical Structure

Motesanib Diphosphate Chemical Structure

CAS No. : 857876-30-3

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ¥1378
In-stock
5 mg ¥1100
In-stock
10 mg ¥1900
In-stock
50 mg ¥5900
In-stock
100 mg ¥9500
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Other Forms of Motesanib Diphosphate:

注册 MCE会员完成审核
即刻享有 积分商城 300 专属积分

Top Publications Citing Use of Products

    Motesanib Diphosphate purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018;48(1):227-236.  [Abstract]

    Immunostaining of CD31 and α-SMA for the analysis of vessel density in infarcted heart.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Motesanib Diphosphate (AMG 706 Diphosphate) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50s of 2 nM/3 nM/6 nM, respectively, and has similar activity against Kit, and is approximately 10-fold more selective for VEGFR than PDGFR and Ret.

    IC50 & Target[1]

    VEGFR1

    2 nM (IC50)

    VEGFR2

    3 nM (IC50)

    VEGFR3

    6 nM (IC50)

    体外研究
    (In Vitro)

    Motesanib Diphosphate (AMG 706 Diphosphate) has broad activity against the human VEGFR family, and displays over 1000-fold selectivity against EGFR, Src, and p38 kinase.Motesanib Diphosphate (AMG 706 Diphosphate) significantly inhibits VEGF-induced cellular proliferation of HUVECs with an IC50 of 10 nM, while displaying little effect at bFGF-induced proliferation with an IC50 of >3,000 nM. Motesanib Diphosphate (AMG 706 Diphosphate) also potently inhibits PDGF-induced proliferation and SCF-induced c-kit phosphorylation with IC50 of 207 nM and 37 nM, respectively, but not effective against the EGF-induced EGFR phosphorylation and cell viability of A431 cells[1]. Although displaying little antiproliferative activity on cell growth of HUVECs alone, Motesanib Diphosphate (AMG 706 Diphosphate) treatment significantly sensitizes the cells to fractionated radiation[2].

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

    体内研究
    (In Vivo)

    Motesanib Diphosphate (AMG 706 Diphosphate) (100 mg/kg) significantly inhibits VEGF-induced vascular permeability in a time-dependent manner. Oral administration of Motesanib twice daily or once daily potently inhibits, in a dose-dependent manner, VEGF-induced angiogenesis using the rat corneal model with ED50 of 2.1 mg/kg and 4.9 mg/kg, respectively. Motesanib Diphosphate (AMG 706 Diphosphate) induces a dose-dependent tumor regression of established A431 xenografts by selectively targeting neovascularization in tumor cells[1]. Motesanib Diphosphate (AMG 706 Diphosphate) in combination with radiation displays significant anti-tumor activity in head and neck squamous cell carcinoma (HNSCC) xenograft models[2]. Motesanib Diphosphate (AMG 706 Diphosphate) treatment also induces significant dose-dependent reductions in tumor growth and blood vessel density of MCF-7, MDA-MB-231, or Cal-51 xenografts, which can be markedly enhanced when combined with docetaxel or tamoxifen[3].

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

    Clinical Trial
    分子量

    569.44

    Formula

    C22H29N5O9P2

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    二磷酸莫替沙尼

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : ≥ 110 mg/mL (193.17 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    H2O 中的溶解度 : 5 mg/mL (8.78 mM; 超声助溶 (<60°C))

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.7561 mL 8.7806 mL 17.5611 mL
    5 mM 0.3512 mL 1.7561 mL 3.5122 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    • 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% Corn Oil

      Solubility: ≥ 25 mg/mL (43.90 mM); 澄清溶液

      此方案可获得 ≥ 25 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 250.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    • 方案 二

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.39 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 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    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)。

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    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
    参考文献
    Kinase Assay
    [1]

    Optimal enzyme, ATP, and substrate (gastrin peptide) concentrations are established for each enzyme using homogeneous time-resolved fluorescence (HTRF) assays. Motesanib is tested in a 10-point dose-response curve for each enzyme using an ATP concentration of two-thirds Km for each. Most assays consist of enzyme mixed with kinase reaction buffer [20 mM Tris-HCl (pH 7.5), 10 mM MgCl2, 5 mM MnCl2, 100 mM NaCl, 1.5 mM EGTA]. A final concentration of 1 mM DTT, 0.2 mM NaVO4, and 20 μg/mL BSA is added before each assay. For all assays, 5.75 mg/mL streptavidin-allophycocyanin and 0.1125 nM Eu-PT66 are added immediately before the HTRF reaction. Plates are incubated for 30 minutes at room temperature and read on a Discovery instrument. IC50 values are calculated using the Levenberg-Marquardt algorithm into a four-parameter logistic equation.

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

    Cell Assay
    [1]

    Cells are preincubated for 2 hours with different concentrations of Motesanib, and exposed with 50 ng/mL VEGF or 20 ng/mL bFGF for an additional 72 hours. Cells are washed twice with DPBS, and plates are frozen at -70°C for 24 hours. Proliferation is assessed by the addition of CyQuant dye, and plates are read on a Victor 1420 workstation. IC50 data are calculated using the Levenberg-Marquardt algorithm into a four-parameter logistic equatio.

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

    Animal Administration
    [1]

    A431 cells are cultured in DMEM (low glucose) with 10% FBS and penicillin/streptomycin/glutamine. Cells are harvested by trypsinization, washed, and adjusted to a concentration of 5×107/mL in serum-free medium. Animals are challenged s.c. with 1×107 cells in 0.2 mL over the left flank. Approximately 10 days thereafter, mice are randomized based on initial tumor volume measurements and treated with either vehicle (Ora-Plus) or Motesanib. Tumor volumes and body weights are recorded twice weekly and/or on the day of sacrifice. Tumor volume is measured with a Pro-Max electronic digital caliper and calculated using the formula length (mm)×width (mm)×height (mm) and expressed in mm3. Data are expressed as mean±SE. Repeated measures ANOVA followed by Scheffe post hoc testing for multiple comparisons is used to evaluate the statistical significance of observed differences[1].

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

    参考文献

    Motesanib Diphosphate 相关分类

    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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 1.7561 mL 8.7806 mL 17.5611 mL 43.9028 mL
    5 mM 0.3512 mL 1.7561 mL 3.5122 mL 8.7806 mL
    DMSO 10 mM 0.1756 mL 0.8781 mL 1.7561 mL 4.3903 mL
    15 mM 0.1171 mL 0.5854 mL 1.1707 mL 2.9269 mL
    20 mM 0.0878 mL 0.4390 mL 0.8781 mL 2.1951 mL
    25 mM 0.0702 mL 0.3512 mL 0.7024 mL 1.7561 mL
    30 mM 0.0585 mL 0.2927 mL 0.5854 mL 1.4634 mL
    40 mM 0.0439 mL 0.2195 mL 0.4390 mL 1.0976 mL
    50 mM 0.0351 mL 0.1756 mL 0.3512 mL 0.8781 mL
    60 mM 0.0293 mL 0.1463 mL 0.2927 mL 0.7317 mL
    80 mM 0.0220 mL 0.1098 mL 0.2195 mL 0.5488 mL
    100 mM 0.0176 mL 0.0878 mL 0.1756 mL 0.4390 mL

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    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.

    您最近查看的产品:

    Your information is safe with us. * Required Fields.

       产品名称:

     

    * 需求量:

    * 客户姓名:

     

    * Email:

    * 电话:

     

    * 公司或机构名称:

       留言给我们:

    Bulk Inquiry

    Inquiry Information

    产品名称:
    Motesanib Diphosphate
    目录号:
    HY-10229
    需求量: