Afatinib

Catalog #: 27009
Size: 10 mg
$110
MW: 485.9 Da
CAS Registry #: 439081-18-2
Formula: C24H25ClFN5O3
Description:
Afatinib, also known as BIW-2992, is an irreversible dual inhibitor of epidermal growth factor receptor 1 (EGFR) and 2 (HER2) tyrosine kinases. Afatinib suppresses EGF-induced EGFR phosphorylation and cellular proliferation in various cell lines, including EGFR-overexpressing and HER2-expressing cell lines A431, NIH-3T3-HER2, NCI-N87 and BT-474.
Synonym(s):
BIW-2992
Purity:

≥95% by HPLC.

Biological Activity:
Afatinib inhibited the EGFR kinase (IC50 = 15 nM) using BPS Bioscience EGFR assay performed using 10 µM ATP and 0.2 mg/ml poly-(Glu-Tyr). Activity was measured by Kinase-Glo Plus reagents (Promega).
Solubility:
Soluble in DMSO at 200 mg/ml; soluble in ethanol at 25 mg/ml; very poorly soluble in water; maximum solubility in plain water is estimated to be about 50-100 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility.
Format:
White crystalline powder.
Storage / Stability:
Store at or below –20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Reference(s):
Eskens, F.A., et al. Br. J. Cancer 98: 80-85 (2008).
Scientific Category:
Kinase
Product Type:
Inhibitor
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Product Datasheets

27009_Lot111121.pdf