| Identification | Back Directory | [Name]
Motesanib | [CAS]
453562-69-1 | [Synonyms]
D06678
CS-1108
motesanib
Motesanib Base
AMG 706; AMG-706
AMG-706(Motesanib)
Motesanib (AMG-706) Base)
N-(3,3-dimethylindolin-6-yl)-2-(pyridin-4-ylmethylamino)nicotinamide
N-(3,3-dimethylindolin-6-yl)-2-(pyridin-4-ylmethylamino)nicotinamide,AMG706
N-(3,3-diMethylindolin-6-yl){2-[(4-pyridylMethyl)-aMino](3-pyridyl)}-carboxaMide
N-(2,3-Dihydro-3,3-dimethyl-1H-indol-6-yl)-2-[(4-pyridinylmethyl)amino]-3-pyridinecarboxamide
3-PyridinecarboxaMide, N-(2,3-dihydro-3,3-diMethyl-1H-indol-6-yl)-2-[(4-pyridinylMethyl)aMino]- | [Molecular Formula]
C22H23N5O | [MDL Number]
MFCD10567689 | [MOL File]
453562-69-1.mol | [Molecular Weight]
373.45 |
| Chemical Properties | Back Directory | [Melting point ]
147-150°C | [Boiling point ]
517.3±50.0 °C(Predicted) | [density ]
1.251 | [storage temp. ]
Refrigerator | [solubility ]
DMSO (Slightly), Methanol (Slightly) | [form ]
White powder solid. | [pka]
11.75±0.40(Predicted) | [color ]
Pale Yellow | [InChI]
InChI=1S/C22H23N5O/c1-22(2)14-26-19-12-16(5-6-18(19)22)27-21(28)17-4-3-9-24-20(17)25-13-15-7-10-23-11-8-15/h3-12,26H,13-14H2,1-2H3,(H,24,25)(H,27,28) | [InChIKey]
RAHBGWKEPAQNFF-UHFFFAOYSA-N | [SMILES]
C1(NCC2C=CN=CC=2)=NC=CC=C1C(NC1=CC2=C(C=C1)C(C)(C)CN2)=O |
| Hazard Information | Back Directory | [Chemical Properties]
Pale Yellow Solid | [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. | [Uses]
Motesanib is an oral angiogenesis inhibitor, demonstrates clinical efficacy in advanced thymoma. | [Definition]
ChEBI:Motesanib is a pyridinecarboxamide. | [Biological Activity]
Motesanib potently inhibits angiogenesis and induces regression in tumor xenografts. | [in vivo]
Motesanib (100 mg/kg) significantly inhibits VEGF-induced vascular permeability in a time-dependent manner. Oral administration of Motesanib twice daily or once daily potently inhibits, in a dose-dependent manner, VEGF-induced angiogenesis using the rat corneal model with ED50 of 2.1 mg/kg and 4.9 mg/kg, respectively. Motesanib induces a dose-dependent tumor regression of established A431 xenografts by selectively targeting neovascularization in tumor cells[1]. Motesanib in combination with radiation displays significant anti-tumor activity in head and neck squamous cell carcinoma (HNSCC) xenograft models[2]. Motesanib treatment also induces significant dose-dependent reductions in tumor growth and blood vessel density of MCF-7, MDA-MB-231, or Cal-51 xenografts, which can be markedly enhanced when combined with docetaxel or tamoxifen[3]. | [target]
VEGFR1 | [IC 50]
VEGFR1: 2 nM (IC50); VEGFR2: 3 nM (IC50); VEGFR3: 6 nM (IC50) | [storage]
Store at -20°C |
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