FIIN 1 hydrochloride 是一种有效的、不可逆的、选择性的 FGFR 抑制剂。 FIIN 1 hydrochloride 与 FGFR1/2/3/4 和 Flt1/4 结合，Kd 分别为 2.8/6.9/5.4/120 nM 和 32/120 nM。 FIIN 1 hydrochloride 对 FGFR1/2/3/4 的生化 IC50 分别为 9.2、6.2、11.9 和 189 nM。
| Cas No. | 1256152-35-8 |
| 别名 | FGFR irreversible inhibitor-1 |
| Canonical SMILES | CCN(CC)CCCCNC1=NC=C2C(N(CC3=CC=CC(NC(C=C)=O)=C3)C(N(C4=C(Cl)C(OC)=CC(OC)=C4Cl)C2)=O)=N1.Cl |
| 分子式 | C32H39Cl2N7O4 |
| 分子量 | 693.06 |
| 溶解度 | Soluble in DMSO |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Potent, irreversible FGFR inhibitor (Kd values are 2.8, 5.4, 6.9 and 120 nM for FGFR1, FGFR3, FGFR2 and FGFR4 respectively); acts at the ATP binding site. Also irreversibly inhibits Flt-1, Flt-4 and VEGFR-2 (Kd values are 32, 120 and 210 nM respectively); displays limited activity (Kd >500 nM) at other kinases. Exhibits antiproliferative activity in FGFR3- and FGFR1-transformed Ba/F3 cells (EC50 values are 10 and 14 nM respectively). Derived from the reversible FGFR inhibitor, PD 173074. Zhou (2010) A structure-guided approach to creating covalent FGFR inhibitors. Chem.Biol. 17 285 PMID:20338520 |
