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

Motesanib (Synonyms: AMG 706; )

目录号: HY-10228 纯度: 99.75%
产品使用指南

Motesanib 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 PDGFR 和 Ret的 10 倍多。

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Motesanib Chemical Structure

Motesanib Chemical Structure

CAS No. : 453562-69-1

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10 mM * 1 mL in DMSO ¥1210 In-stock
5 mg ¥1100 In-stock
10 mg ¥1900 In-stock
50 mg ¥5900 In-stock
100 mg ¥9500 In-stock
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Customer Review

Other Forms of Motesanib:

Top Publications Citing Use of Products

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

    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

    Description

    Motesanib 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 appr 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)

    In Vitro

    Motesanib has broad activity against the human VEGFR family, and displays > 1000 selectivity against EGFR, Src, and p38 kinase. Motesanib 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 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]. Althouth displaying little antiproliferative activity on cell growth of HUVECs alone, Motesanib treatment significantly sensitizes the cells to fractionated radiation[2]

    In Vivo

    Motesanib (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 induces a dose-dependent tumor regression of established A431 xenografts by selectively targeting neovascularization in tumor cells[1]. Motesanib in combination with radiation displays significant anti-tumor activity in head and neck squamous cell carcinoma (HNSCC) xenograft models[2]. Motesanib 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]

    Clinical Trial
    Molecular Weight

    373.45

    Formula

    C₂₂H₂₃N₅O

    CAS No.

    453562-69-1

    SMILES

    O=C(C1=CC=CN=C1NCC2=CC=NC=C2)NC3=CC(NCC4(C)C)=C4C=C3

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 30 mg/mL (80.33 mM)

    * "≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.6777 mL 13.3887 mL 26.7773 mL
    5 mM 0.5355 mL 2.6777 mL 5.3555 mL
    10 mM 0.2678 mL 1.3389 mL 2.6777 mL
    *

    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。 -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。

    References
    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.

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

    References

    Purity: 99.75%

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    Keywords:

    MotesanibAMG 706AMG706AMG-706c-KitVEGFRSCFRCD117Vascular endothelial growth factor receptorInhibitorinhibitorinhibit

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    目录号:
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