For research use only. Not for therapeutic Use.
Mubritinib (TAK-165) is a potent and selective EGFR2/HER2 inhibitor with an IC50 of 6 nM.
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)[1].
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[1].
| Catalog Number | I003349 |
| CAS Number | 366017-09-6 |
| Synonyms | 4-[[4-[4-(triazol-1-yl)butyl]phenoxy]methyl]-2-[(E)-2-[4-(trifluoromethyl)phenyl]ethenyl]-1,3-oxazole |
| Molecular Formula | C25H23F3N4O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C25H23F3N4O2/c26-25(27,28)21-9-4-20(5-10-21)8-13-24-30-22(18-34-24)17-33-23-11-6-19(7-12-23)3-1-2-15-32-16-14-29-31-32/h4-14,16,18H,1-3,15,17H2/b13-8+ |
| InChIKey | ZTFBIUXIQYRUNT-MDWZMJQESA-N |
| SMILES | C1=CC(=CC=C1CCCCN2C=CN=N2)OCC3=COC(=N3)C=CC4=CC=C(C=C4)C(F)(F)F |
| Reference | [1]. Nagasawa J, et al. Novel HER2 selective tyrosine kinase inhibitor, TAK-165, inhibits bladder, kidney and androgen-independent prostate cancer in vitro and in vivo. Int J Urol. 2006 May;13(5):587-92. |
