tcsc0691 Falnidamol

Falnidamol (BIBX 1382) is a potent, selective inhibitor of EGFR tyrosine kinase (IC₅₀ = 3 nM); displays > 1000-fold lower potency against ErbB2 (IC₅₀ = 3.4 μM) and a range of other related tyrosine kinases (IC₅₀ > 10 μM).

IC50 & Target: IC50: 3 nM (EGFR)^[1].

In Vitro: Falnidamol (BIBX 1382) and BIBU1361 are both potent and selective submicromolar inhibitors of the EGFR kinase activity. An IC₅₀ value of 3 nM was determined for both compounds. The potency of these two compounds compares with the one obtained with Iressa, which is a leading EGFR inhibitor in the field. Inhibition of the closest family member, HER2, was 100- to 1000-fold less potent. Furthermore, Falnidamol (BIBX 1382) and BIBU1361 did not inhibit a number of other related tyrosine kinases^[1].

In Vivo: In nude mice, oral once daily dosing at 10 mg/kg with either Falnidamol (BIBX 1382) or BIBU1361 completely suppressed tumor growth of human A431 xenografts with respective T/C values of 15 and 6% after 2 weeks of treatment^[1].