| Identification | Back Directory | [Name]
AMG-706 | [CAS]
857876-30-3 | [Synonyms]
CS-459
AMG-706
Unii-T6Q3060U91
Diphosphate salt
AMG-706 USP/EP/BP
Motesanib(AMG-706)
Motesanib phosphate
Motesanib diphosphate
AMG706; AMG 706; AMG-706
Motesanib, Diphosphate Salt
Motesanib diphosphate [usan]
AMG706 (Motesanib Diphosphate)
Motesanib Diphosphate (AMG-706)
AMG706;AMG 706;AMG-706;MOTESANIB
Motesanib Diphosphate (AMG-706) VM-2005
N-(2,3-Dihydro-3,3-diMethyl-1H-indol-6-yl)-2-[(4-pyridinylMethyl)aMino]-3-pyridinecarboxaMide Phosphate
N-(3,3-dimethyl-1,2-dihydroindol-6-yl)-2-(pyridin-4-ylmethylamino)pyridine-3-carboxamide,phosphoric acid
N-(2,3-Dihydro-3,3-dimethyl-1H-indol-6-yl)-2-[(4-pyridinylmethyl)amino]-3-pyridinecarboxamide diphosphate
3-Pyridinecarboxamide, N-(2,3-dihydro-3,3-dimethyl-1H-indol-6-yl)-2-[(4-pyridinylmethyl)amino]-, phosphate (1:2) | [Molecular Formula]
C22H29N5O9P2 | [MDL Number]
MFCD27978100 | [MOL File]
857876-30-3.mol | [Molecular Weight]
569.441 |
| Chemical Properties | Back Directory | [storage temp. ]
Inert atmosphere,Store in freezer, under -20°C | [solubility ]
≥28.45 mg/mL in DMSO; insoluble in H2O; ≥3.47 mg/mL in EtOH with ultrasonic | [form ]
Powder | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
An oral angiogenesis inhibitor, demonstrates clinical efficacy in advanced thymoma. | [Uses]
Motesanib Diphosphate (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3, PDGFR, c-Kit and Ret with IC50 of 2 nM/3 nM/6 nM, 84 nM, 8 nM and 59 nM, respectively. | [Biological Activity]
motesanib diphosphate is a diphosphate form of motesanib. it is a potent atp-competitive inhibitor of vegfr1/2/3 with ic50 of 2 nm/3 nm/6 nm, respectively [1].vascular endothelial growth factor (vegf) is an important signaling protein involved in both vasculogenesis (the formation of the circulatory system) and angiogenesis (the growth of blood vessels from pre-existing vasculature). motesanib (amg 706) is an orally administered small molecule belonging to angiokinase inhibitor class which acts as an antagonist of vegf receptors, platelet-derived growth factor receptors, and stem cell factor receptors. | [in vitro]
motesanib diphosphate has broad activity against the human vegfr family, and displays >1000 selectivity against egfr, src, and p38 kinase. 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 also potently inhibits pdgf-induced proliferation and scf-induced c-kit phosphorylation with ic50 of 207 nm and 37 nm, respectively, but not effective against the egf-induced egfr phosphorylation and cell viability of a431 cells [1]. althouth displaying little antiproliferative activity on cell growth of huvecs alone, motesanib diphosphate treatment significantly sensitizes the cells to fractionated radiation [2]. | [in vivo]
oral administration of amg 706 potently inhibited vegf-induced angiogenesis in the rat corneal model and induced regression of established a431 xenografts. amg 706 was well tolerated and had no significant effects o amg 706n body weight or on the general health of the animals. histologic analysis of tumor xenografts from amg 706–treated animals revealed an increase in endothelial apoptosis and a reduction in blood vessel area that preceded an increase in tumor cell apoptosis. in summary, amg 706 is an orally bioavailable, well-tolerated multikinase inhibitor that is presently under clinical investigation for the treatment of human malignancies [1]. | [target]
VEGFR | [IC 50]
VEGFR1: 2 nM (IC50); VEGFR2: 3 nM (IC50); VEGFR3: 6 nM (IC50) | [storage]
Store at -20°C |
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