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CAS No. : 366017-09-6
MCE 国际站:Mubritinib
产品活性:Mubritinib (TAK-165) 是有效,选择性的 EGFR2/HER2 抑制剂,IC50 值为6 nM。
研究领域:JAK/STAT Signaling | Protein Tyrosine Kinase/RTK
作用靶点:EGFR
In Vitro: Mubritinib (TAK-165) specifically inhibits HER2 tyrosine kinase with an IC50 6 nM and does not inhibit other types tyrosine kinase up to 25 000 nM. Mubritinib inhibits HER2 phosphorylation and its down-stream Akt and MAPK in HER2 strongly expressing cells (BT474 breast cancer cell line). Mubritinib sensitivity depends on HER2 levels of each cell line. Especially, BT474 cells which over-express HER2 strongly is highly sensitive (IC50=0.005 µM) and PC-3 cells which express HER2 very weakly is less sensitive (IC50=4.62 µM). But, HT1376 and ACHN cells that over-expressed EGFR showed high IC50 (IC50>25 µM).
In Vivo: In the xenograft model, treatment with Mubritinib (TAK-165) significantly inhibits growth of UMUC-3, ACHN, and LN-REC4. The antitumor effect after 14 days treatment are 22.9%, 26.0%, and 26.5% in UMUC3, ACHN and LN-REC4, respectively.
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