Erlotinib · HCl
EGFR Kinase inhibitor / Potent inhibitor of EGFR tyrosine kinase (IC50 = 2 nM)1. Potent inhibitor of mutant JAK2-V617F2. Weaker inhibitor of ErbB-2 kinase (Ki = 1 μM) ErbB-4 kinase (Ki = 1.5 μM)3. HDAC inhibitors sensitize for erlotinib activity in EGFR-mutated and wildtype non-small cell lung cancer (NSCLC) cells4. A clinically effective agent for NSCLC5.
Biochemicals & reagents
183319-69-9
1) Moyer et al. (1997), Induction of apoptosis and cell cycle arrest by CP-358,774, an inhibitor of epidermal growth factor tyrosine kinases; Cancer Res, 57 4838 2) Li et al. (2007), Erlotinib effectively inhibits JAK2V617F activity and polycythemia vera cell growth; J. Biol. Chem., 282 3428 3) Wood et al. (2004), A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells; Cancer Res., 64 6652 4) Greve et al. (2015), The pan-HDAC inhibitor panobinostat acts as a sensitizer for erlotinib activity in EGFR-mutated and –wildtype non-small cell lung cancer cells; BMC Cancer, 15 947 5) Minquet et al. (2016), Targeted therapies for treatment of non-small cell lung cancer-Recent advances and future perspectives; Int. J. Cancer, 138 2549
-20°C
TARGET: Kinase -- PATHWAY: EGF; JAK/STAT -- DISEASE AREA: Cancer