Erlotinib Hydrochloride

Inhibitor of the epidermal growth factor receptor tyrosine kinase, which is highly expressed and occasionally mutated in various forms of cancer. Erlotinib binds reversibly to the ATP binding site of the receptor.\n\nSolubility:\nSoluble in DMSO at 18mg/ml with warming; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 5-20uM; buffers, serum, or other additives may increase or decrease the aqueous solubility.\n\nElemental Analysis (Calculated):\nC: 61.46%\nH: 5.63%\nCl: 8.25%\nN: 9.77%\n\nStorage and Stability:\nMay be stored at RT for short-term only. Long-term storage is recommended at -20 degrees C. Stable for 6 months. For maximum recovery of product, centrifuge the original vial prior to removing the cap.

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SPECIFICATIONS

Catalog Number

E3452-75

Size

1g

Form

Supplied as a white to off-white powder.

Purity

HPLC, TLC: ~99%

References

1. Raymond, E., et al. \"Epidermal growth factor receptor tyrosine kinase as a target for anticancer therapy.\" Drugs 60 Suppl 1:15-23, discussion 41-42 (2000). 2. Moyer, J.D., et al. \"Induction of Apoptosis and Cell Cycle Arrest by erlotinib, an Inhibitor of Epidermal Growth Factor Receptor Tyrosine Kinase.\" Cancer Res. 57:4838-4848 (1997). 3. Li, Z., et al. \"Erlotinib effectively inhibits JAK2V617F activity and polycythemia vera cell growth.\" J. Biol. Chem. 282:3428-3432 (2007). 4. Wood, E.R., et al. \"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. 64:6652-6659 (2004).