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Amuvatinib
- MP 470
- Soluble in DMSO
- MF: C23H21N5O3S
- MW: 447.51
Description
Amuvatinib (MP470) is a receptor tyrosine kinase inhibitor that inhibits PDGFR, c-Kit and c-Met in the low-micromolar range and modulates survival and DNA repair proteins including pAKT, RAD51 and GSK-3β. It inhibits proliferation, induces growth arrest and promotes apoptosis in prostate cancer models.
RTK signaling and DNA repair pathways cooperate to support tumor-cell survival and therapy resistance. Amuvatinib is useful for studying multi-RTK inhibition, RAD51-associated repair modulation and combination approaches with EGFR/HER-family pathway inhibitors. The combination of Amuvatinib and Erlotinib (Axon 1128) suppresses prostate cancer tumor growth by fully disrupting the HER family/PI3K/Akt pathway.
Key Features
- Multi-target RTK inhibitor
- Inhibits PDGFR, c-Kit and c-Met in reported assays
- Modulates pAKT, RAD51 and GSK-3β
- Promotes growth arrest and apoptosis in prostate cancer cells
Applications
- Receptor tyrosine kinase pharmacology
- DNA repair and RAD51 studies
- Prostate cancer model research
- Combination therapy mechanism assays
More Information
| Parent CAS No. | 850879-09-3 |
|---|---|
| Chemical Name | N-(Benzo[d][1,3]dioxol-5-ylmethyl)-4-(benzofuro[3,2-d]pyrimidin-4-yl)piperazine-1-carbothioamide |
| SMILES | N1(C(=S)NCC2=CC=C3OCOC3=C2)CCN(C2N=CN=C3C4=CC=CC=C4OC3=2)CC1 |
| MFCD | MFCD16038298 |
| InChi | InChI=1S/C23H21N5O3S/c32-23(24-12-15-5-6-18-19(11-15)30-14-29-18)28-9-7-27(8-10-28)22-21-20(25-13-26-22)16-3-1-2-4-17(16)31-21/h1-6,11,13H,7-10,12,14H2,(H,24,32) |
| InChiKey | FOFDIMHVKGYHRU-UHFFFAOYSA-N |
| CID | 11282283 |
| Short Description | RTK inhibitor |
References
- W. Qi et al. MP470, a novel receptor tyrosine kinase inhibitor, in combination with Erlotinib inhibits the HER family/PI3K/Akt pathway and tumor growth in prostate cancer. BMC Cancer. 2009, 9, 142.
- D. Mahadevan et al. A novel tyrosine kinase switch is a mechanism of imatinib resistance in gastrointestinal stromal tumors. Oncogene. 2007, , 26, 3909-3919.
- C.J. Phillip et al. Targeting MET kinase with the small-molecule inhibitor amuvatinib induces cytotoxicity in primary myeloma cells and cell lines. J. Hematol. Oncol. 2013, 6, 1-16.
- J.W. Welsh et al. The c-Met receptor tyrosine kinase inhibitor MP470 radiosensitizes glioblastoma cells. Radiat. Oncol. 2009, 4, 69.
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