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Mubritinib
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Mubritinib
CAS No. : 366017-09-6
MCE 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 ?M) and PC-3 cells which express HER2 very weakly is less sensitive (IC50=4.62 ?M). But, HT1376 and ACHN cells that over-expressed EGFR showed high IC50 (IC50>25 ?M).
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.
相关产品:Clinical Compound Library Plus | Bioactive Compound Library Plus | Immunology/Inflammation Compound Library | JAK/STAT Compound Library | Kinase Inhibitor Library | Protein Tyrosine Kinase Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Differentiation Inducing Compound Library | Anti-Hepatitis C Virus Compound Library | Anti-Breast Cancer Compound Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Gefitinib | Trastuzumab | Erlotinib | Cetuximab | AG490 | Genistein | AG-1478 | Pertuzumab | BI-4020 | NSC 228155 | Pelitinib | TX1-85-1 | Canertinib | Butein | PD168393 | Daphnetin | EGFR-IN-7 | AEE788 | Chrysophanol | PD153035 | Tyrphostin 23 | Lavendustin A | Trastuzumab emtansine | BMS-599626 Hydrochloride | PD158780 | AV-412
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热门标签:TAK-165