产品介绍
Product Description
General description
A cell-permeable 4,6-dianilinopyrimidine compound that acts as a potent, ATP-competitive, and highly selective inhibitor of EGFR and some EGFR mutants (IC50 = 21 nM, 63 nM, and 4 nM for EGFRwt, EGFRL858R and EGFRL861Q, respectively) vs. erbB4/Her4 (IC50 = 7.64 µM) and a panel of 55 other kinases. Shown to completely block EGF-induced EGFR autophosphorylation in U-2OS cells at 10 µM.
Biochem/physiol Actions
Cell permeable: yes
Product competes with ATP.
Reversible: no
Target IC50: 21 nM, 63 nM, and 4 nM for EGFRwt, EGFRL858R and EGFRL861Q, respectively
Packaging
Packaged under inert gas
Other Notes
Zhang, Q., et al. 2006. J. Am. Chem. Soc.128, 2182
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
技术参数
Specifications
| Quality Level | 100 |
| assay | ≥97% (HPLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | off-white |
| solubility | ethanol: 25 mg/mL,DMSO: 50 mg/mL |
| shipped in | ambient |
| storage temp. | −20°C |
| SMILES string | FC(F)(F)c1cc(ccc1)Nc2ncnc(c2)Nc3cc(ccc3)NC(=O)C4CC4 |
| InChI | 1S/C21H18F3N5O/c22-21(23,24)14-3-1-4-15(9-14)27-18-11-19(26-12-25-18)28-16-5-2-6-17(10-16)29-20(30)13-7-8-13/h1-6,9-13H,7-8H2,(H,29,30)(H2,25,26,27,28) |
| InChI key | YOHYSYJDKVYCJI-UHFFFAOYSA-N |
