eCF506是高效，有口服活性的非受体酪氨酸激酶 Src 的抑制剂， IC₅₀ 值小于0.5 nM。

eCF506 is a highly potent and orally bioavailable inhibitor of the non-receptor tyrosine kinase Src with an IC 50 of less than 0.5 nM.

Solid

IC50: less than 0.5 nM (Src)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

eCF506 shows a moderate oral bioavailability (25.3%). A significant reduction of phospho-SRC is observed in the xenograft sections from mice treated with eCF506 relative to the untreated animal controls. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Fraser C, et al. Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. J Med Chem. 2016 May 26;59(10):4697-710.

In Vitro: DMSO : 62.5 mg/mL (122.40 mM; Need ultrasonic)H₂O : < 0.1 mg/mL (insoluble)配制储备液