Afatinib

  • Chemical Properties
CAS No. 850140-72-6 Cat. No. BCP04467
Name Afatinib
Synonyms Gilotrif;Tovok;BIBW2992;BIBW-2992;BIBW 2992;(2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide;
Formula C24H25ClFN5O3 M. Wt 485.94
  • Biological Activity
Description BIBW2992 shows potent activity against both wild-type and mutant forms of EGFR and HER2. It is similar to Gefitinib in potency against L858R EGFR, but about 100-fold more active against the Gefitinib resistant L858R-T790M EGFR double mutant. BIBW2992 exhibits potent effects on both EGFR and HER2 phosphorylation in vivo. It compares favorably to reference compounds (such as Lapatinib et al.) in all cell types tested, such as human epidermoid carcinoma cell line A431 expressing wt EGFR, murine NIH-3T3 cells transfected with wt HER2, as well as breast cancer cell line BT-474 and gastric cancer cell line NCI-N87, which express endogenous HER2.
Related Products 439081-18-2(Afatinib) 850140-73-7(Afatinib dimaleate)
Pathways Angiogenesis/Protein Tyrosine Kinase Jak/Stat Pathway 
Targets EGFR HER2 

Structure

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