| Name | Motesanib Diphosphate |
| Description | Motesanib Diphosphate (AMG 706) is the orally bioavailable diphosphate salt of a multiple-receptor tyrosine kinase inhibitor with potential antineoplastic activity. |
| Cell Research | Cells are preincubated for 2 hours with different concentrations of Motesanib Diphosphate, 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(Only for Reference) |
| Kinase Assay | In vitro kinase assays: Optimal enzyme, ATP, and substrate (gastrin peptide) concentrations are established for each enzyme using homogeneous time-resolved fluorescence (HTRF) assays. Motesanib Diphosphate 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. |
| In vitro | In a rat corneal model, administering Motesanib Diphosphate orally twice daily (ED50=2.1 mg/kg) or once daily (ED50=4.9 mg/kg) effectively inhibited vascular endothelial growth factor-induced angiogenesis. Additionally, in a model of transplanted squamous cell carcinoma of the head and neck, the combined use of Motesanib Diphosphate and radiation therapy demonstrated significant anticancer activity. |
| In vivo | In human umbilical vein endothelial cells (HUVECs) induced by VEGF (IC50=10 nM), Motesanib Diphosphate significantly inhibits cell proliferation. It also markedly suppresses proliferation prompted by platelet-derived growth factor (IC50=207 nM) and c-kit phosphorylation induced by SCF (IC50=37 nM). Additionally, Motesanib Diphosphate enhances the sensitivity of these cells to radiation and exhibits broad-spectrum activity against the human VEGFR family. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : 16 mg/mL (28.1 mM), Sonication is recommended.
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 93 mg/mL (163.32 mM), Sonication is recommended.
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| Keywords | VEGFR3 | VEGFR2/Flk1 | VEGFR2 | VEGFR1 | VEGFR | Vascular endothelial growth factor receptor | SCFR | Motesanib Diphosphate | Kit | Inhibitor | inhibit | c-Kit | cKit | CD117 | AMG-706 | AMG706 | AMG 706 Diphosphate |
| Inhibitors Related | Ribociclib | Gilteritinib | Nintedanib | Regorafenib monohydrate | Sorafenib | Pexidartinib | Regorafenib | Sorafenib tosylate | Lenvatinib mesylate | Imatinib | Pazopanib | Axitinib |
| Related Compound Libraries | Reprogramming Compound Library | Failed Clinical Trials Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
