Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Motesanib Diphosphate (AMG 706) is the orally bioavailable diphosphate salt of a multiple-receptor tyrosine kinase inhibitor with potential antineoplastic activity.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
5 mg | In stock | $ 36.00 | |
10 mg | In stock | $ 52.00 | |
25 mg | In stock | $ 97.00 | |
50 mg | In stock | $ 171.00 | |
100 mg | In stock | $ 297.00 | |
500 mg | In stock | $ 728.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 54.00 |
Description | Motesanib Diphosphate (AMG 706) is the orally bioavailable diphosphate salt of a multiple-receptor tyrosine kinase inhibitor with potential antineoplastic activity. |
Targets&IC50 | c-Kit:8 nM, VEGFR2/Flk1:6 nM, VEGFR1:2 nM, VEGFR3:6 nM, VEGFR2:3 nM |
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. |
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. |
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) |
Synonyms | Motesanib, AMG 706 |
Molecular Weight | 569.44 |
Formula | C22H23N5O·2H3PO4 |
CAS No. | 857876-30-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 16 mg/mL (28.1 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 93 mg/mL (163.3 mM)
You can also refer to dose conversion for different animals. More
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Motesanib Diphosphate 857876-30-3 Angiogenesis Tyrosine Kinase/Adaptors VEGFR c-Kit Motesanib AMG-706 inhibit AMG 706 Diphosphate Vascular endothelial growth factor receptor AMG706 SCFR Inhibitor AMG 706 CD117 inhibitor