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Motesanib

Catalog No. T2288 CAS 453562-69-1

Synonyms: AMG 706

Motesanib (AMG 706) is an orally bioavailable receptor tyrosine kinase inhibitor with potential antineoplastic activity. AMG 706 selectively targets and inhibits vascular endothelial growth factor (VEGFR), platelet-derived growth factor (PDGFR), Kit, and Ret receptors, thereby inhibiting angiogenesis and cellular proliferation.

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Motesanib, CAS 453562-69-1

Pack Size	Availability	Price/USD
5 mg	In stock	$ 37.00
10 mg	In stock	$ 54.00
50 mg	In stock	$ 174.00
1 mL * 10 mM (in DMSO)	In stock	$ 58.00

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Purity: 98.87%

Purity: 98.26%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Motesanib (AMG 706) is an orally bioavailable receptor tyrosine kinase inhibitor with potential antineoplastic activity. AMG 706 selectively targets and inhibits vascular endothelial growth factor (VEGFR), platelet-derived growth factor (PDGFR), Kit, and Ret receptors, thereby inhibiting angiogenesis and cellular proliferation.
Targets&IC50	c-Kit:8 nM, VEGFR1:2 nM, VEGFR3:6 nM, VEGFR2:3 nM
In vitro	Motesanib exhibits extensive efficacy against the VEGFR family in humans, with more than 1000-fold selectivity over EGFR, Src, and p38 kinase. It notably reduces VEGF-triggered proliferation in HUVECs, achieving an IC50 of 10 nM, but demonstrates minimal influence on bFGF-driven proliferation, with an IC50 exceeding 3,000 nM. Furthermore, Motesanib effectively hinders PDGF-stimulated proliferation and SCF-induced c-kit phosphorylation, presenting IC50 values of 207 nM and 37 nM, respectively. However, it lacks efficacy against EGF-induced EGFR phosphorylation and the viability of A431 cells. While having limited antiproliferative effects on HUVECs growth on its own, Motesanib markedly enhances the sensitivity of these cells to fractionated radiation.
In vivo	Motesanib, at a dose of 100 mg/kg, significantly reduces VEGF-induced vascular permeability in a time-dependent manner. When administered orally once or twice daily, it effectively suppresses VEGF-induced angiogenesis in the rat corneal model, with ED50 values of 4.9 mg/kg and 2.1 mg/kg, respectively. Furthermore, Motesanib promotes dose-dependent regression of established A431 xenografts by targeting tumor cell neovascularization. In combination with radiation, it demonstrates pronounced anti-tumor efficacy in head and neck squamous cell carcinoma (HNSCC) xenograft models. Additionally, Motesanib alone, or when combined with docetaxel or tamoxifen, significantly curtails tumor growth and blood vessel density in MCF-7, MDA-MB-231, or Cal-51 xenografts in a dose-dependent manner.
Kinase Assay	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.
Cell Research	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.

Synonyms	AMG 706
Molecular Weight	373.45
Formula	C22H23N5O
CAS No.	453562-69-1

Storage

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

Solubility Information

DMSO: 100 mM

References and Literature

1. Polverino A, et al. AMG 706, an oral, multikinase inhibitor that selectively targets vascular endothelial growth factor, platelet-derived growth factor, and kit receptors, potently inhibits angiogenesis and induces regression in tumor xenografts. Cancer R 2. Kruser TJ, et al. Augmentation of radiation response by motesanib, a multikinase inhibitor that targets vascular endothelial growth factor receptors. Clin Cancer Res, 2010, 16(14), 3639-3647. 3. Coxon A, et al. Broad antitumor activity in breast cancer xenografts by motesanib, a highly selective, oral inhibitor of vascular endothelial growth factor, platelet-derived growth factor, and Kit receptors. Clin Cancer Res, 2009, 15(1), 110-118.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Inhibitor Library Anti-Cancer Drug Library Tyrosine Kinase Inhibitor Library Anti-Cancer Active Compound Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Angiogenesis related Compound Library Anti-Liver Cancer Compound Library Bioactive Compounds Library Max

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SU5408 Alectinib JNJ-38158471 Parsatuzumab JI-101 SU14813 maleate Motesanib Diphosphate Lucitanib

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Keywords

Motesanib 453562-69-1 Angiogenesis Tyrosine Kinase/Adaptors VEGFR c-Kit inhibit AMG-706 SCFR AMG 706 Vascular endothelial growth factor receptor CD117 AMG706 Inhibitor inhibitor

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