Mubritinib
Mubritinib Basic information
- Product Name:
- Mubritinib
- Synonyms:
-
- MUBRITINIB
- 1-(4-(4-((2-((1E)-2-(4-(Trifluoromethyl)phenyl)ethenyl)-4-oxazolyl)methoxy)phenyl)butyl)-1H-1,2,3-triazole
- TAK 165
- Mubritinib(TAK 165)
- CS-522
- TAK165;TAK-165
- (E)-1-(4-(4-((2-(4-(trifluoromethyl)styryl)oxazol-4-yl)methoxy)phenyl)butyl)-1H-1,2,3-triazole
- 1-(4-(4-((2-((1E)-2-(4-(Trifluoromethyl)phenyl)ethenyl)-4-oxazolyl)methoxy)phenyl)butyl)-1H-1,2,3-triazole Mubritinib (TAK 165)
- CAS:
- 366017-09-6
- MF:
- C25H23F3N4O2
- MW:
- 468.47
- Product Categories:
-
- Inhibitors
- Mol File:
- 366017-09-6.mol
Mubritinib Chemical Properties
- Melting point:
- 158.0 to 162.0 °C
- Boiling point:
- 620.9±65.0 °C(Predicted)
- Density
- 1.25±0.1 g/cm3(Predicted)
- storage temp.
- Store at +4°C
- solubility
- DMSO : 50 mg/mL (106.73 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)
- pka
- 1.45±0.10(Predicted)
- form
- powder to crystal
- color
- White to Gray to Brown
- 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
- N1(CCCCC2=CC=C(OCC3=COC(/C=C/C4=CC=C(C(F)(F)F)C=C4)=N3)C=C2)C=CN=N1
Mubritinib Usage And Synthesis
Uses
Treatment of cancer.
Uses
Mubritinib is used in selective targeting of CTNNB1-, KRAS-or MYC-driven human cancer cell growth by combinations of existing drugs
Biological Activity
Potent, irreversible human epithelial growth factor receptor 2 (ErbB2) inhibitor (IC 50 = 6 nM) that displays > 4000-fold selectivity over EGFR, FGFR, PDGFR, JAK1 and Src. Exhibits potent antiproliferative effects in ErbB2-overexpressing cancer cell lines (IC 50 = 5 nM in BT474 breast cancer cells) and significantly inhibits bladder, breast and prostate cancer xenograft growth in vivo .
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[1].
IC 50
HER2: 6 nM (IC50)
storage
Store at +4°C
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