Motesanib Diphosphate

SKU: orb1704443

Description

Motesanib Diphosphate (AMG 706) is an orally administered small molecule that inhibits multiple receptor tyrosine kinases. It has been investigated in preclinical cancer research for its anti-angiogenic and anti-tumor effects in both in vitro assays and in vivo xenograft models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 857876-30-3
• MW: 569.44
• Purity: 99.76%
• Formula: C₂₂H₂₃N₅O·2H₃PO₄
• SMILES: OP(=O)(O)O.CC1(C)CNc2c1ccc(NC(=O)c1c(NCc3ccncc3)nccc1)c2.OP(=O)(O)O
• Target: c-Kit,VEGFR
• Solubility: H2O:16 mg/mL (28.1 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (5.8 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:93 mg/mL (163.32 mM)

Bioactivity

• Target IC50:
  VEGFR2/Flk1:6 nM|c-Kit:8 nM|VEGFR2:3 nM|VEGFR3:6 nM|VEGFR1:2 nM
• 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.
• 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.
• 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)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AMG 706, AMG 706 Diphosphate, AMG706, AMG-706, CD117, c-Kit, cKit, Kit, inhibit, Motesanib, Motesanib Diphosphate, Inhibitor, SCFR, Vascular endothelial growth factor receptor, VEGFR2, VEGFR1, VEGFR, VEGFR3, VEGFR2/Flk1

Compound Identifiers

PubChem CID

16097729