| Identification | Back Directory | [Name]
2-Propenamide, N-[3-[[3-(3,5-dimethoxyphenyl)-3,4-dihydro-7-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-2-oxopyrimido[4,5-d]pyrimidin-1(2H)-yl]methyl]phenyl]- | [CAS]
2093088-81-2 | [Synonyms]
2-Propenamide, N-[3-[[3-(3,5-dimethoxyphenyl)-3,4-dihydro-7-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-2-oxopyrimido[4,5-d]pyrimidin-1(2H)-yl]methyl]phenyl]- | [Molecular Formula]
C35H38N8O4 | [MOL File]
2093088-81-2.mol | [Molecular Weight]
634.73 |
| Chemical Properties | Back Directory | [density ]
1.306±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 10mg/mL, clear | [form ]
powder | [pka]
13.54±0.70(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Description]
FIIN-4 is a first-in-class covalent inhibitor of FGFR (Fibroblast Growth Factor Receptor) that inhibits metastatic breast cancer. Structurally, FIIN-4 is an regional isomer of FIIN-2 (Cat#406652). FIIN-4 effectively blocks 3D metastatic outgrowth as compared with currently available FGFR inhibitors. In vivo application of FIIN-4 potently inhibited the growth of metastatic, patient-derived breast cancer xenografts and murine-derived metastases growing within the pulmonary microenvironment. (Copied from Mol Cancer Ther. 2016 Sep;15(9):2096-106. ) | [Uses]
FIIN-4 is a first-in-class, orally active and covalent FGFR inhibitor with IC50s of 2.6 nM, 2.6 nM, 5.6 nM, 9.2 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. FIIN-4 can inhibit metastatic tumor growth. | [References]
[1] Wells S Brown, et al. Covalent Targeting of Fibroblast Growth Factor Receptor Inhibits Metastatic Breast Cancer. Mol Cancer Ther. 2016 Sep;15(9):2096-106. DOI:10.1158/1535-7163.MCT-16-0136 |
|
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|