afatinib-hcl

Description: Afatinib impurity 11 is a major impurity of Afatinib which is a potent and orally bioavailable dual receptor tyrosine kinase (RTK) inhibitor. Afatinib is an FDA approved anticancer drug used to treat non-small cell lung carcinoma (NSCLC). It is sold under the brand name of Gilotrif in the USA. It irreversibly binds to and inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM in cell-free assays, respectively; and is 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant.

References: Oncogene. 2008 Aug 7; 27(34):4702-11; Br J Cancer. 2008 Jan 15; 98(1):80-5.

Related CAS: 850140-72-6 (Afatinib free base); 850140-73-7 (Afatinib dimaleate)