产品说明
生化/生理作用
FIIN-4 is 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.
基本信息
| 经验(实验)分子式 | C35H38N8O4 |
| 分子量 | 634.73 |
| NACRES | NA.77 |
产品性质
| 质量水平 | 100 |
| 测定 | ≥98% (HPLC) |
| 形式 | powder |
| 储存条件 | protect from light |
| 颜色 | white to beige |
| 溶解性 | DMSO: 10 mg/mL, clear |
| 储存温度 | 2-8℃ |
安全信息
| 储存分类代码 | 13 - Non Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
