eCF506

1914078-41-3

C26H38N8O3

H2O : < 0.1 mg/mL (insoluble); DMSO : 62.5 mg/mL (122.40 mM; Need ultrasonic)

Protein Tyrosine Kinase/RTK

eCF506 is a highly potent and orally bioavailable inhibitor of the non-receptor tyrosine kinase Src with an IC₅₀ of less than 0.5 nM. IC50 & Target: IC50: less than 0.5 nM (Src)^[1] In Vitro: eCF506 induces a very potent antiproliferative effect in both MCF7 and MDA-MB-231 cells. eCF506 inhibits phosphorylation of SRC and FAK at low nanomolar levels, with complete inhibition observed at 100 nM. eCF506 significantly reduces cell motility at 10 nM as early as 6 h into the study, with equivalent efficacy to dasatinib. eCF506 exclusively inhibits SFK, with subnanomolar IC₅₀ values against SRC and YES (IC₅₀=0.5, 2.1 nM). It is important to highlight that eCF506 displays a vast difference in activity (>950-fold difference) between ABL and its primary target SRC^[1]. In Vivo: eCF506 shows a moderate oral bioavailability (25.3%). A significant reduction of phospho-SRC^Y416 is observed in the xenograft sections from mice treated with eCF506 relative to the untreated animal controls^[1].