Motesanib (Diphosphate)

Motesanib (Diphosphate)

• CAS Number: 857876-30-3
• UNSPSC Description: Motesanib Diphosphate (AMG 706 Diphosphate) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50s of 2 nM/3 nM/6 nM, respectively, and has similar activity against Kit, and is approximately 10-fold more selective for VEGFR than PDGFR and Ret.
• Target Antigen: c-Kit; VEGFR
• Type: Reference compound
• Related Pathways: Protein Tyrosine Kinase/RTK
• Applications: Cancer-Kinase/protease
• Field of Research: Cancer
• Assay Protocol: https://www.medchemexpress.com/Motesanib-Diphosphate.html
• Purity: 99.64
• Solubility: DMSO : ≥ 110 mg/mL|H2O : 5 mg/mL (ultrasonic;warming;heat to 60°C)
• Smiles: O=C(C1=CC=CN=C1NCC2=CC=NC=C2)NC3=CC(NCC4(C)C)=C4C=C3.O=P(O)(O)O.O=P(O)(O)O
• Molecular Weight: 569.44
• References & Citations: [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 Res. 2006 Sep 1;66(17):8715-21.|[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.Oncotarget. 2016 Sep 27;7(39):63839-63855.|Cell Physiol Biochem. 2018;48(1):227-236. |Harvard Medical School LINCS LIBRARY|J Cell Biochem. 2020 Mar;121(3):2343-2353.|Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.
• Shipping Conditions: Room Temperature
• Storage Conditions: 4°C (Powder, sealed storage, away from moisture)
• Clinical Information: Phase 3