tcsc0100 Dasatinib

Dasatinib (BMS-354825) is a dual Bcr-Abl and Src family tyrosine kinase inhibitor with IC₅₀s of 0.6, 0.8, 79 and 37 nM for Abl, Src, c-Kit and c-Kit^D816V, respectively.

IC50 & Target: IC50: 0.6 nM/0.8 nM (Abl^WT/Src)^[1]


IC50: 79 nM/37 nM (c-Kit^WT/c-Kit^D816V)^[2]

In Vitro: Dasatinib potently inhibits wild-type Abl kinase and all mutants except T315I over a narrow range (IC₅₀≤1.7 nM). Dasatinib (IC₅₀: 0.8 nM) displays 325-fold greater potency compared with Imatinib against cells expressing wild-type Bcr-Abl in Ba/F3 cells^[1].

In Vivo: Daily treatment with Dasatinib (50 mg/kg) is initiated on day 10. Using this approach, a significant inhibition of BCPAP orthotopic tumor growth is observed 6 days after treatment (day 16, P=0.014), which is sustained through days 23 and 29 (P=0.0003), compared with vehicle-treated mice^[3]. Metabolism studies of Dasatinib (50 mg/kg) in rat suggested that Dasatinib is the major circulating component, whereas multiple metabolites contributed to the remaining 40-60% of the sample radioactivity at 4 h post dose^[4].