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Submit ReviewErlotinib Hydrochloride
Description: Potent, reversible EGFR tyrosine kinase inhibitor
Chemical Name: N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride
Purity: ≥98% (HPLC)
Biological Activity for Erlotinib Hydrochloride
Erlotinib hydrochloride is a reversible, potent EGFR tyrosine kinase inhibitor (IC50 = 2 nM); it reduces EGFR autophosphorylation in intact tumor cells (IC50 = 20 nM). Erlotinib is selective for cell lines showing PC-9 and H3255 mutations (IC50 values are 7 and 12 nM, respectively, sparing wild-type and T790 mutant EGFR. Erlotinib shows antiproliferative effects in cancer cell lines in vitro and promotes differentiation of urothelial organoids. Orally bioavailable.
Compound Libraries for Erlotinib Hydrochloride
Erlotinib Hydrochloride is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
Technical Data for Erlotinib Hydrochloride
| M. Wt | 429.9 |
| Formula | C22H23N3O4.HCl |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 183319-69-9 |
| PubChem ID | 176871 |
| InChI Key | GTTBEUCJPZQMDZ-UHFFFAOYSA-N |
| Smiles | Cl.C#CC1=CC=CC(=C1)NC=2N=CN=C3C=C(OCCOC)C(OCCOC)=CC32 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Erlotinib Hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 8.6 | 20 |
Preparing Stock Solutions for Erlotinib Hydrochloride
The following data is based on the product molecular weight 429.9. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 11.63 mL | 58.15 mL | 116.31 mL |
| 1 mM | 2.33 mL | 11.63 mL | 23.26 mL |
| 2 mM | 1.16 mL | 5.82 mL | 11.63 mL |
| 10 mM | 0.23 mL | 1.16 mL | 2.33 mL |
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Product Datasheets for Erlotinib Hydrochloride
References for Erlotinib Hydrochloride
References are publications that support the biological activity of the product.
Santos et al (2019) Urothelial organoids originating from Cd49fhigh mouse stem cells display Notch-dependent differentiation capacity. Nat.Commun. 10 PMID: 31562298
Moyer et al (1997) Induction of apoptosis and cell cycle arrest by CP-358,774, an inhibitor of epidermal growth factor receptor tyrosine kinase. Cancer Res. 57 4838 PMID: 9354447
If you know of a relevant reference for Erlotinib Hydrochloride, please let us know.
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Keywords: Erlotinib Hydrochloride, Erlotinib Hydrochloride supplier, erlotinib, HCl, hydrochloride, potent, reversible, EGFR, tyrosine, kinase, inhibitors, inhibits, epidermal, growth, factor, receptor, antiproliferative, organoids, differentiation, Organoids, 7194, Tocris Bioscience
Citations for Erlotinib Hydrochloride
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Cancer Research Product Guide
A collection of over 750 products for cancer research, the guide includes research tools for the study of:
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- Receptor Signaling
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A collection of over 400 products for kinase research, the listing includes inhibitors of:
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- Protein Kinases A, C, D and G
- PI-3 Kinase, Akt and mTOR
- MAPK Signaling
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