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Erlotinib HCl | EGFR Kinase inhibitor

Erlotinib HCl (182219-93-9) is a potent inhibitor of EGFR tyrosine kinase (IC50 = 2 nM).1 Potent inhibitor of mutant JAK2-V617F.2 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) cells.4 A clinically effective agent for NSCLC.5


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

Focus Biomolecules supplier, chemical structure of Erlotinib HCl | EGFR Kinase inhibitor | CAS 183319-69-9

Catalog#  10-2135

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Catalog Number:
EGFR Kinase inhibitor
Chemical Name:
N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine hydrochloride
Molecular Weight:
Molecular Formula:
C22H23N3O4 HCl
Soluble in DMSO (up to 18 mg/ml with warming).
Physical Properties:
White or off-white solid
98% by TLC
NMR (Conforms)
Storage Temperature:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
Shipping Code:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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