Mubritinib

Research use only, not for human use.

Mubritinib (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM.

Mubritinib, also known as TAK-165, is a protein kinase inhibitor which was under development by Takeda for the treatment of cancer. It completed phase I clinical trials (may be discontinued since 2008). Mubritinib(TAK 165) is a potent EGFR, HER2 and p34cdc2 inhibitor with IC50 of 6 nM and 0.2 μM, respectively. Mubritinib(TAK 165) also inhibits p33cdk2 and p33cdk5. Mubritinib(TAK 165) displays > 4000-fold selectivity over EGFR, FGFR, PDGFR, JAK1 and Src. Mubritinib(TAK 165) exhibits potent antiproliferative effects in ErbB2-overexpressing cancer cell lines (IC50 = 5 nM in BT474 breast cancer cells) and significantly inhibits bladder, breast and prostate cancer xenograft growth in vivo.

Mubritinib; TAK 165; TAK-165

Membrane Transporter/Ion Channel

TRP/TRPV Channel

EGFR; HER2/ErbB2; FGFR; JAK1; PDGFR

Cancer

——

366017-09-6

468.47

C25H23F3N4O2

98%

DMSO : 50 mg/mL 106.73 mM; H2O : < 0.1 mg/mL

c1cc(ccc1CCCCn1ccnn1)OCc1coc(n1)/C=C/c1ccc(cc1)C(F)(F)F

(E)-4-((4-(4-(1H-1,2,3-triazol-1-yl)butyl)phenoxy)methyl)-2-(4-(trifluoromethyl)styryl)oxazole

(-20℃)

With Ice Pack

≥ 2 years