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eCF506

CAS No. : 1914078-41-3

MCE 国际站：eCF506

产品活性：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。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Src

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.

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.

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