Motesanib
Motesanib
CAS: 453562-69-1
Molecular Formula: C22H23N5O
Motesanib - Names and Identifiers
| Name | Motesanib |
| Synonyms | AMG 706 CS-1108 AMG-706 motesanib Motesanib Motesanib Base AMG-706(Motesanib) Motesanib (AMG-706) Base) 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 N-(3,3-dimethyl-2,3-dihydro-1H-indol-6-yl)-2-[(pyridin-4-ylmethyl)amino]pyridine-3-carboxamide 3-PyridinecarboxaMide, N-(2,3-dihydro-3,3-diMethyl-1H-indol-6-yl)-2-[(4-pyridinylMethyl)aMino]- |
| CAS | 453562-69-1 |
| InChI | InChI=1/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) |
Motesanib - Physico-chemical Properties
| Molecular Formula | C22H23N5O |
| Molar Mass | 373.45 |
| Density | 1.251 |
| Melting Point | 147-150°C |
| Boling Point | 517.3±50.0 °C(Predicted) |
| Flash Point | 266.628°C |
| Solubility | DMSO |
| Vapor Presure | 0mmHg at 25°C |
| Appearance | White powder solid. |
| Color | Pale Yellow |
| pKa | 11.75±0.40(Predicted) |
| Storage Condition | Refrigerator |
| Refractive Index | 1.669 |
| Use | An inhibitor of Flk-1, Flt-4, PDGFR-β and c-Kit. |
| In vitro study | Motesanib has broad activity against the human VEGFR family, and displays > 1000 selectivity against EGFR, Src, and p38 kinase. Motesanib significantly inhibits VEGF-induced cellular proliferation of HUVECs with an IC 50 of 10 nM, while displaying little effect at bFGF-induced proliferation with an IC 50 of >3,000 nM. Motesanib also potently inhibits PDGF-induced proliferation and SCF-induced c-kit phosphorylation with IC 50 of 207 nM and 37 nM, respectively, but not effective against the EGF-induced EGFR phosphorylation and cell viability of A431 cells.Althouth displaying little antiproliferative activity on cell growth of HUVECs alone, Motesanib treatment significantly sensitizes the cells to fractionated radiation. |
| In vivo study | 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 ED 50 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. Motesanib in combination with radiation displays significant anti-tumor activity in head and neck squamous cell carcinoma (HNSCC) xenograft models.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. |
Motesanib - Introduction
Motesanib (AMG-706) is an ATP competitive VEGFR1,2,3 inhibitor with IC50 of 2 nM,3 nM and 6 nM, respectively, and 8 nM for c-Kit.
Last Update：2022-10-16 17:25:17
Motesanib - Reference Information
| introduction | Motesanib is an effective ATP competitive inhibitor of VEGFR1/2/3, with an IC50 value of 2 nM/3 nM/6 nM, similar to the selectivity to Kit, more than 10 times that of PDGFR and Ret. |
| use | Motesenyi, also known as AMG-706, is a multi-kinase inhibitor that can selectively target VEGF receptors, platelet-derived growth factor receptors (PDGFRs) and Kit receptors, with ICΩ values of 2 nM(VEGFR1) and 3 nM(VEGFR2), respectively, 6 nM (VEGFR3),84 nM(PDGFR) and 8 nM(Kit). It also effectively inhibited angiogenesis and induced regression of xenotumours. Motesenib is an inhibitor of Flk-1, Flt-4, PDGFR-and c-Kit. |
| biological activity | Motesanib (AMG-706) is an orally bioactive receptor tyrosine kinase (receptor tyrosine kinase) inhibitor, which is resistant to VEGFR1, VEGFR2, VEGFR3, Kit, IC50 values for PDGFR and Ret were 2, 3, 6, 8, 84 and 59 nM, respectively. |
| target | TargetValue VEGFR1 (Cell-Free Assay) 2 nM VEGFR2 (Cell-Free Assay) 3 nM VEGFR3 (Cell-Free Assay) 6 nM c-Kit (Cell-Free Assay) 8 nM c-Kit (Cell-Free Assay) 8 nM |
| Target | Value |
| VEGFR1 (Cell-free assay) | 2 nM |
| VEGFR2 (Cell-free assay) | 3 nM |
| VEGFR3 (Cell-free assay) | 6 nM |
| c-Kit (Cell-free assay) | 8 nM 8 nM |
| in vitro study | Motesanib has broad activity against the human VEGFR family, and displays > 1000 selectivity against EGFR, Src, and p38 kinase. Motesanib significantly inhibits VEGF-induced cellular proliferation of HUVECs with an IC 50 of 10 nM, while displaying little effect at bFGF-induced proliferation with an IC 50 of >3,000 nM. Motesanib also potently inhibits PDGF-induced proliferation and SCF-induced c-kit phosphorylation with IC 50 of 207 nM and 37 nM, respectively, but not effective against the EGF-induced EGFR phosphorylation and cell viability of A431 cells.Althouth displaying little antiproliferative activity on cell growth of HUVECs alone, Motesanib treatment significantly sensitizes the cells to fractionated radiation. |
| in vivo study | 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 pose-dependent manner, VEGF-induced angiogenesis using the rat corneal model with ed 50 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. Motesanib in combination with radiation displays significant anti-tumor activity in head and neck squamous cell carcinoma (HNSCC) xenograft models.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. |
Last Update：2024-04-09 21:01:54
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