Product nameErlotinib hydrochloride, EGFR tyrosine kinase inhibitor
DescriptionPotent EGFR tyrosine kinase inhibitor
- Erlotinib HCl
Potent EGFR tyrosine kinase inhibitor (IC50 = 2 nM). Decreases EGFR autophosphorylation in tumor cells. Potent inhibitor of mutant JAK2-V617F. Weaker inhibitor of ErbB-2 kinase (Ki = 1 μM) and ErbB-4 kinase (Ki = 1.5 μM). Clinically effective agent for non-small cell lung cancer (NSCLC).
Chemical nameN-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine hydrochloride
Storage instructionsShipped at Room Temperature. Store at -20°C. Store under desiccating conditions.
Solubility overviewSoluble in DMSO to 25 mM (with warming)
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
This product has been referenced in:
- Minguet J et al. Targeted therapies for treatment of non-small cell lung cancer--Recent advances and future perspectives. Int J Cancer 138:2549-61 (2016). Read more (PubMed: 26537995) »
- Greve G et al. 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 (2015). Read more (PubMed: 26675484) »
- Griffero F et al. Different response of human glioma tumor-initiating cells to epidermal growth factor receptor kinase inhibitors. J Biol Chem 284:7138-48 (2009). Read more (PubMed: 19147502) »
- Li Z et al. Erlotinib effectively inhibits JAK2V617F activity and polycythemia vera cell growth. J Biol Chem 282:3428-32 (2007). Read more (PubMed: 17178722) »
- Minna JD & Dowell J Erlotinib hydrochloride. Nat Rev Drug Discov Suppl:S14-5 (2005). Read more (PubMed: 15962526) »
- Moyer JD et al. Induction of apoptosis and cell cycle arrest by CP-358,774, an inhibitor of epidermal growth factor receptor tyrosine kinase. Cancer Res 57:4838-48 (1997). Read more (PubMed: 9354447) »