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Motesanib diphosphate (AMG 706) is a novel oral inhibitor of VEGF receptors, platelet-derived growth-factor receptor, and KIT. It is used as the phosphate salt motesanib diphosphate. Motesanib Diphosphate significantly inhibits VEGF-induced cellular proliferation of HUVECs with an IC50 of 10 nM, while displaying little effect at bFGF-induced proliferation with an IC50 of >3,000 nM. Motesanib Diphosphate (AMG 706) induces a dose-dependent tumor regression of established A431 xenografts by selectively targeting neovascularization in tumor cells. Motesanib diphosphate (AMG 706) can induce partial responses in patients with advanced or metastatic differentiated thyroid cancer that is progressive.
| Molecular Weight | 569.44 |
| Formula | C22H23N5O.2H3PO4 |
| CAS Number | 857876-30-3 |
| Solubility (25°C) | DMSO 100 mg/mL Water 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related VEGFR/PDGFR Products |
|---|
| ABT-869
ABT-869 (Linifanib) is an ATP-competitive, multi-targeted RTK inhibitor that is completely effective against all members of VEGFR and PDGFR. |
| Tivozanib (AV-951)
Tivozanib (AV-951) is a potent VEGFR-1, 2 and 3, c-Kit and PDGFR inhibitor with IC50 of 0.21, 0.16, 0.24, 1.63 and 1.72 nM respectively. |
| Axitinib
Axitinib (AG013736) inhibits multiple targets including VEGFR, PDGFR and cKit. |
| Regorafenib
Regorafenib (BAY 73-4506) is a novel oral multikinase inhibitor of c-KIT, VEGFR2, B-Raf with IC50s of 17, 40 and 69 nM respectively. |
| Nintedanib
Nintedanib (BIBF1120) is a novel, potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively. |
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