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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 2.0 Max and 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
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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:
- Cancer Metabolism
- Epigenetics in Cancer
- Receptor Signaling
- Cell Cycle and DNA Damage Repair
- Angiogenesis
- Invasion and Metastasis
Angiogenesis in Cancer Poster
Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.