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EOC317

CAS No. : 939805-30-8

MCE 国际站：EOC317

产品活性：EOC317 (ACTB-1003) 是口服可用的激酶抑制剂，抑制 FGFR1，VEGFR2 和 Tie-2 的 IC₅₀ 值分别为6，2 和 4 nM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：FGFR  |  VEGFR

In Vitro: EOC317 (ACTB-1003) is an oral kinase inhibitor with multiple modes of action, targeting cancer mutations via FGFR inhibition FGFR1 (IC₅₀=6 nM), angiogenesis through inhibition of VEGFR2 (2 nM), Tie-2 (4 nM), and induces apoptosis likely by targeting RSK (5 nM) and p70S6K (32 nM). EOC317 is highly active with dose-dependent tumor growth inhibition in cell lines with FGFR genetic alterations-OPM2 human multiple myeloma and the murine leukemia Ba/F3-TEL-FGFR1. OPM2 cells harbor the FGFR3 t(4:14) translocation, FGFR3 K650E mutation and PTEN deletion while the Ba/F3-TEL-FGFR1 cells are driven by FGFR1 over-expression.

In Vivo: EOC317 (ACTB-1003) is shown to inhibit tumor angiogenesis evident by the inhibition of CD31 staining in tumor sections. EOC317 is combinable with 5-FU or paclitaxel without diminishing the activity or increasing the toxicity of these chemotherapy agents in the HCT-116 colon tumor xenograft model.

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