Falnidamol NLT 98%

Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC₅₀ of 3 nM. Falnidamol displays > 1000-fold lower potency against ErbB2 (IC₅₀=3.4 μM) and a range of other related tyrosine kinases (IC₅₀>10 μM). Falnidamol is a pyrimido-pyrimidine compound and has anti-cancer activity^[1][2]. In Vitro: Falnidamol (BIBX 1382) demonstrates antiproliferative activity in mitogenic assays performed with KB cells^[2].
In Vivo: Falnidamol (BIBX 1382; p.o.; 10 mg/kg/day; 16 days) completely suppressed tumor growth of human A431 xenografts with respective a T/C value of 15% after 2 weeks of treatment^[2].
Falnidamol (50 mg/kg/day for 2 weeks) results in dephosphorylation of the EGF receptor in A431 xenograft-bearing mice^[2].
With Falnidamol (p.o.; 10 mg/kg/day; 16 days), the C_4h is 2222 nM and the C_24h is 244 nM^[2].