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Motesanib Diphosphate

Catalog No. T2288L CAS 857876-30-3

Synonyms: Motesanib, AMG 706

Motesanib Diphosphate (AMG 706) is the orally bioavailable diphosphate salt of a multiple-receptor tyrosine kinase inhibitor with potential antineoplastic activity.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Motesanib Diphosphate Chemical Structure

Motesanib Diphosphate, CAS 857876-30-3

Pack Size	Availability	Price/USD
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

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Purity: 99.76%

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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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 16 mg/mL (28.1 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 93 mg/mL (163.3 mM)

References and Literature

1. Polverino A, et al. Cancer Res, 2006, 66(17), 8715-8721. 2. Kruser TJ, et al. Clin Cancer Res, 2010, 16(14), 3639-3647. 3. Coxon A, et al. Clin Cancer Res, 2009, 15(1), 110-118.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library Human Metabolite Library Anti-Breast Cancer Compound Library Anti-Ovarian Cancer Compound Library

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Keywords

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

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