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
Warning
Toxicity: Standard Handling (A)
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
Molecular Weight: 413.40. Empirical Formula: C21H18F3N5O. 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. 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. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 51182303
- Condition:
- New
- HazmatClass:
- No
- MPN:
- 324674-1MG
- CAS:
- 879127-07-8
akash.verma@cenmed.com
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