For research use only. Not for therapeutic Use.
Amuvatinib（Cat No.:I005106）is a multi-targeted tyrosine kinase inhibitor that primarily targets c-Kit, PDGFR, and FLT3, all of which are critical in tumor cell proliferation and survival. It has shown potential in treating various cancers, including small cell lung cancer (SCLC) and gastrointestinal stromal tumors (GIST), especially in cases resistant to other therapies. Amuvatinib also enhances the activity of DNA-damaging agents by inhibiting DNA repair enzymes, making it a promising candidate for combination cancer therapies. Its ability to target multiple pathways offers a versatile approach to tackling drug-resistant tumors.
| Catalog Number | I005106 |
| CAS Number | 850879-09-3 |
| Synonyms | N-(1,3-benzodioxol-5-ylmethyl)-4-([1]benzofuro[3,2-d]pyrimidin-4-yl)piperazine-1-carbothioamide |
| Molecular Formula | C₂₃H₂₁N₅O₃S |
| Purity | ≥95% |
| Target | c-RET |
| Solubility | DMSO ≥30mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL |
| Storage | 3 years -20℃ powder |
| IC50 | 10 nM(c-KitD816H); 40 nM(PDGFRαV561D); 81 nM(Flt3D835Y) |
| IUPAC Name | N-(1,3-benzodioxol-5-ylmethyl)-4-([1]benzofuro[3,2-d]pyrimidin-4-yl)piperazine-1-carbothioamide |
| 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 |
| SMILES | C1CN(CCN1C2=NC=NC3=C2OC4=CC=CC=C43)C(=S)NCC5=CC6=C(C=C5)OCO6 |
| Reference | </br>1:Erratum to: Targeting MET kinase with the small-molecule inhibitor amuvatinib induces cytotoxicity in primary myeloma cells and cell lines. Phillip CJ, Zaman S, Shentu S, Balakrishnan K, Zhang J, Baladandayuthapani V, Taverna P, Redkar S, Wang M, Stellrecht CM, Gandhi V.J Hematol Oncol. 2016 Oct 13;9(1):110. No abstract available. PMID: 27737688 Free PMC Article</br>2:Amuvatinib has cytotoxic effects against NRAS-mutant melanoma but not BRAF-mutant melanoma. Fedorenko IV, Fang B, Koomen JM, Gibney GT, Smalley KS.Melanoma Res. 2014 Oct;24(5):448-53. doi: 10.1097/CMR.0000000000000103. PMID: 24950457 Free PMC Article</br>3:Phase 1B study of amuvatinib in combination with five standard cancer therapies in adults with advanced solid tumors. Mita M, Gordon M, Rosen L, Kapoor N, Choy G, Redkar S, Taverna P, Oganesian A, Sahai A, Azab M, Bristow R, Tolcher AW.Cancer Chemother Pharmacol. 2014 Jul;74(1):195-204. doi: 10.1007/s00280-014-2481-1. Epub 2014 May 22. PMID: 24849582 </br>4:Targeting MET kinase with the small-molecule inhibitor amuvatinib induces cytotoxicity in primary myeloma cells and cell lines. Phillip CJ, Zaman S, Shentu S, Balakrishnan K, Zhang J, Baladandayuthapani V, Taverna P, Redkar S, Wang M, Stellrecht CM, Gandhi V.J Hematol Oncol. 2013 Dec 10;6:92. doi: 10.1186/1756-8722-6-92. Erratum in: J Hematol Oncol. 2016 Oct 13;9(1):110. PMID: 24326130 Free PMC Article</br>5:A phase I, first-in-human dose-escalation study of amuvatinib, a multi-targeted tyrosine kinase inhibitor, in patients with advanced solid tumors. Tibes R, Fine G, Choy G, Redkar S, Taverna P, Oganesian A, Sahai A, Azab M, Tolcher AW.Cancer Chemother Pharmacol. 2013 Feb;71(2):463-71. doi: 10.1007/s00280-012-2019-3. Epub 2012 Nov 23. PMID: 23178951 </br>6:Safety, tolerability, and pharmacokinetics of amuvatinib from three phase 1 clinical studies in healthy volunteers. Choy G, Joshi-Hangal R, Oganesian A, Fine G, Rasmussen S, Collier J, Kissling J, Sahai A, Azab M, Redkar S.Cancer Chemother Pharmacol. 2012 Jul;70(1):183-90. doi: 10.1007/s00280-012-1821-2. Epub 2012 Feb 15. PMID: 22349808 </br>7:The receptor tyrosine kinase inhibitor amuvatinib (MP470) sensitizes tumor cells to radio- and chemo-therapies in part by inhibiting homologous recombination. Zhao H, Luoto KR, Meng AX, Bristow RG.Radiother Oncol. 2011 Oct;101(1):59-65. doi: 10.1016/j.radonc.2011.08.013. Epub 2011 Sep 6. PMID: 21903282 |
