AMG-706 (Motesanib) is an orally-available, nicotinamide-based, ATP-competitive inhibitor of the VEGFR family of kinases, KIT, and PDGFR with IC50s of 2, 3, and 6 nM, 8 nM, and 84 nM (for VEGFR1, VEGFR2, and VEGFR3), respectively. Besides Ret activity (IC50 = 59 nM), AMG-706 is highly selective against other unrelated kinases, including Src and EGFR. [1] AMG-706 potently inhibits VEGF-induced proliferation of HUVECs with IC50 values of 10 nM. PDGF-induced proliferation and SCF-induced c-Kit phosphorylation was also inhibited at IC50 values of 207 and 37 nM, respectively.
AMG-706 was shown to increase tumor response to radiation in UM-SCC1 and SCC-1483 xenografts of head and neck squamous cell carcinomas. [2]
Technical information:
| Chemical Formula: | C22H23N5O.2H3PO4 | |
| CAS #: | 453562-69-1 | |
| Molecular Weight: | 569.44 | |
| Purity: | >98% | |
| Appearance: | White | |
| Chemical Name: | 3-Pyridinecarboxamide, N-(2,3-dihydro-3,3-dimethyl-1H-indol-6-yl)-2-[(4-pyridinylmethyl)amino]- | |
| Solubility: | Up to 100mM in DMSO | |
| Synonyms: | AMG-706, AMG 706, AMG706, Motesanib |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Polverino 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 Res. 2006, 66, 8715-8721. Pubmed ID: 16951187 |
| 2. | Kruser et al., Augmentation of radiation response by motesanib, a multikinase inhibitor that targets vascular endothelial growth factor receptors. Clin. Cancer Res. 2010, 16, 3639-3647. Pubmed ID: 20507929 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
