Motesanib - CAS 453562-69-1
Catalog number:
453562-69-1
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C22H23N5O
Molecular Weight:
373.45
COA:
Inquire
Targets:
c-Kit
Description:
Motesanib is a multikinase inhibitor that selectively targets VEGF receptors, platelet-derived growth factor receptors (PDGFRs), and Kit receptors. It also potently inhibits angiogenesis and induces regression in tumor xenografts.
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Purity:
>98%
Related CAS:
453562-69-1 (Motesanib); 857876-30-3 (Motesanib diphosphate)
Appearance:
White to off-white solid powder
Synonyms:
N-(3,3-dimethyl-2,3-dihydro-1H-indol-6-yl)-2-[(pyridin-4- ylmethyl)amino]pyridine-3-carboxamide; AMG 706; AMG706; AMG706; motesanib
MSDS:
Inquire
InChIKey:
RAHBGWKEPAQNFF-UHFFFAOYSA-N
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)
Canonical SMILES:
O=C(C1=CC=CN=C1NCC2=CC=NC=C2)NC3=CC4=C(C=C3)C(C)(C)CN4
1.Effects of a Multikinase Inhibitor Motesanib (AMG 706) Alone and Combined with the Selective DuP-697 COX-2 Inhibitor on Colorectal Cancer Cells.
Kaya TT1, Altun A, Turgut NH, Ataseven H, Koyluoglu G. Asian Pac J Cancer Prev. 2016;17(3):1103-10.
In the present study, we investigated the effects of motesanib (AMG 706), a multikinase inhibitor alone and in combination with DuP-697, an irreversible selective inhibitor of COX-2, on cell proliferation, angiogenesis, and apoptosis induction in a human colorectal cancer cell line (HT29). Real time cell analysis (RTCA, Xcelligence system) was used to determine the effects on colorectal cancer cell proliferation. Apoptosis was assessed with annexin V staining and angiogenesis was determined with chorioallantoic membrane model. We found that motesanib alone exerted antiproliferative, antiangiogenic and apoptotic effects on HT29 colorectal cancer cells. Combination with DUP-697 increased the antiproliferative, antiangiogenic and apoptotic effects. Results of this study indicate that motesanib may be a good choice in treatment of colorectal tumors. In addition, the increased effects of combination of motesanib with DuP-697 raise the possibility of using lower doses of these drugs and therefore avoid/minimize the dose-dependent side effects generally observed.
2.High Affinity Pharmacological Profiling of Dual Inhibitors Targeting RET and VEGFR2 in Inhibition of Kinase and Angiogeneis Events in Medullary Thyroid Carcinoma.
Dunna NR1, Kandula V, Girdhar A, Pudutha A, Hussain T, Bandaru S, Nayarisseri A. Asian Pac J Cancer Prev. 2015;16(16):7089-95.
Clinical evidence shows that dual inhibition of kinases as well angiogenesis provides ideal therapeutic option in the treatment of medullary thyroid carcinoma (MTC) than inhibiting either of these with the events separately. Although treatment with dual inhibitors has shown good clinical responses in patients with MTC, it has been associated with serious side effects. Some inhibitors are active agents for both angiogenesis or kinase activity. Owing to narrow therapeutic window of established inhibitors, the present study aims to identify high affinity dual inhibitors targeting RET and VEGFR2 respectively for kinase and angiogenesis activity. Established inhibitors like Vandetanib, Cabozantinib, Motesanib, PP121, RAF265 and Sunitinib served as query parent compounds for identification of structurally similar compounds by Tanimoto-based similarity searching with a threshold of 95% against the PubChem database. All the parent inhibitors and respective similar compounds were docked against RET and VEGFR2 in order to retrieve high affinity compounds with these two proteins.
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