For research use only. Not for therapeutic Use.
AMG-925（Cat No.:I001528）is a dual inhibitor targeting both FLT3 and CDK4/6 kinases, designed to treat acute myeloid leukemia (AML) and other hematologic malignancies. By simultaneously inhibiting FLT3, a receptor tyrosine kinase involved in leukemic cell proliferation, and CDK4/6, critical regulators of the cell cycle, AMG-925 offers a comprehensive approach to blocking cancer cell growth and survival. This dual-action mechanism enhances its efficacy in overcoming resistance often seen in single-target therapies.
| Catalog Number | I001528 |
| CAS Number | 1401033-86-0 |
| Molecular Formula | C₂₆H₂₉N₇O₂ |
| Purity | ≥95% |
| Target | Cyclin-Dependent Kinases |
| Solubility | DMSO: ＜ 10 mM |
| Storage | Store at -20℃ |
| IC50 | 1.5/2.4 nM (CDK4/FLT3) |
| IUPAC Name | 2-hydroxy-1-[2-[[8-(4-methylcyclohexyl)-4,6,8,11-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaen-5-yl]amino]-7,8-dihydro-5H-1,6-naphthyridin-6-yl]ethanone |
| InChI | InChI=1S/C26H29N7O2/c1-16-2-5-18(6-3-16)33-22-13-27-10-8-19(22)20-12-28-26(31-25(20)33)30-23-7-4-17-14-32(24(35)15-34)11-9-21(17)29-23/h4,7-8,10,12-13,16,18,34H,2-3,5-6,9,11,14-15H2,1H3,(H,28,29,30,31) |
| InChIKey | BBUVDDPUURMFOX-UHFFFAOYSA-N |
| SMILES | CC1CCC(CC1)N2C3=C(C=CN=C3)C4=CN=C(N=C42)NC5=NC6=C(CN(CC6)C(=O)CO)C=C5 |
| Reference | </br>1:AMG 925 is a dual FLT3/CDK4 inhibitor with the potential to overcome FLT3 inhibitor resistance in acute myeloid leukemia. Li C, Liu L, Liang L, Xia Z, Li Z, Wang X, McGee LR, Newhall K, Sinclair A, Kamb A, Wickramasinghe D, Dai K.Mol Cancer Ther. 2015 Feb;14(2):375-83. doi: 10.1158/1535-7163.MCT-14-0388. Epub 2014 Dec 8. PMID: 25487917 Free Article</br>2:Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3. Li Z, Wang X, Eksterowicz J, Gribble MW Jr, Alba GQ, Ayres M, Carlson TJ, Chen A, Chen X, Cho R, Connors RV, DeGraffenreid M, Deignan JT, Duquette J, Fan P, Fisher B, Fu J, Huard JN, Kaizerman J, Keegan KS, Li C, Li K, Li Y, Liang L, Liu W, Lively SE, Lo MC, Ma J, McMinn DL, Mihalic JT, Modi K, Ngo R, Pattabiraman K, Piper DE, Queva C, Ragains ML, Suchomel J, Thibault S, Walker N, Wang X, Wang Z, Wanska M, Wehn PM, Weidner MF, Zhang AJ, Zhao X, Kamb A, Wickramasinghe D, Dai K, McGee LR, Medina JC.J Med Chem. 2014 Apr 24;57(8):3430-49. doi: 10.1021/jm500118j. Epub 2014 Apr 2. PMID: 24641103 </br>3:Preclinical evaluation of AMG 925, a FLT3/CDK4 dual kinase inhibitor for treating acute myeloid leukemia. Keegan K, Li C, Li Z, Ma J, Ragains M, Coberly S, Hollenback D, Eksterowicz J, Liang L, Weidner M, Huard J, Wang X, Alba G, Orf J, Lo MC, Zhao S, Ngo R, Chen A, Liu L, Carlson T, Quéva C, McGee LR, Medina J, Kamb A, Wickramasinghe D, Dai K.Mol Cancer Ther. 2014 Apr;13(4):880-9. doi: 10.1158/1535-7163.MCT-13-0858. Epub 2014 Feb 13. PMID: 24526162 Free Article |
