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Mubritinib

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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