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View larger FIIN-4
AOBS1956
CAS No: 2093088-81-2
Chemical Name: N-(3-((3-(3,5-dimethoxyphenyl)-7-((4-(4-methylpiperazin-1-yl)phenyl)amino)-2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidin-1(2H)-yl)methyl)phenyl)acrylamide
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Quantity Discount Table - Order More To Get More Price Discount
| Quantity | mg | Unit Price ($/mg or $/Unit) | Final Price |
|---|---|---|---|
| 1 | 5 | $22.95 | Total: $114.75 |
| 1 | 10 | $19.44 | Total: $194.40 |
| 1 | 25 | $16.47 | Total: $411.75 |
| 1 | 50 | $14.04 | Total: $702.00 |
| 1 | 100 | $12.15 | Total: $1,215.00 |
Data sheet
| Molecular Formula | C35H38N8O4 |
| Molecular Weight | 634.74 |
| CAS Numbers | 2093088-81-2 |
| Storage Condition | 0°C (short term), -20°C (long term), desiccated |
| Solubility | DMSA: 10 mg/mL |
| Purity | 98% by HPLC |
More info
A potent, irreversible, type II inhibitor against FGFR (IC50 = 2.6, 2.6, 5.6, 9.2 nM, respectively, against FGFR1-4) whose 4-acrylamidebenzyl moiety covalently modifies FGFR P-loop cysteine in its DFG-out conformation with good target selectivity based on a 456-kinase panel (354 non-mutants kinases) kinome profiling. FIIN-4 effectively inhibits FGF2-induced Erk1/2 phosphorylation in serum-starved D2.A1 murine mammary carcinoma cells (by 100% wtih 18-hr 250 nM pretreatment) and D2.A1 growth in 3D cultures (by 54% at 100 nM) without affecting EGF-dependent Erk phosphorylation or 3D growth of NMuMG murine mammary epithelial cells. Oral administration (25 mg/kg q.o.d.) is efficacious in suppressing the growths of tumors-derived from murine mammary carcinoma 4T1 lung metastases and patient TNBC brain metastases xenografts in mice in vivo with good pharmacokinetics (Tmax = 0.5 hr, T1/2 = 2.4 hr, AUC = 935 h·ng/mL; 10 mg/kg p.o.) and without overt toxicity to the animals.