Mubritinib
Mubritinib
CAS: 366017-09-6
Molecular Formula: C25H23F3N4O2
Mubritinib - Names and Identifiers
| Name | Mubritinib |
| Synonyms | TAK165 CS-522 TAK-165 TAK 165 MUBRITINIB Mubritinib Mubritinib(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 1-(4-{4-[(2-{(E)-2-[4-(trifluoromethyl)phenyl]ethenyl}-1,3-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 |
| InChI | InChI=1/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+ |
Mubritinib - Physico-chemical Properties
| Molecular Formula | C25H23F3N4O2 |
| Molar Mass | 468.47 |
| Density | 1.25±0.1 g/cm3(Predicted) |
| Melting Point | 158.0 to 162.0 °C |
| Boling Point | 620.9±65.0 °C(Predicted) |
| Flash Point | 329.3°C |
| Solubility | Soluble in DMSO (25 mg/mL) with warming; ethanol (1.7 mg/mL), and water (<1 mg/mL). |
| Vapor Presure | 2.43E-15mmHg at 25°C |
| Appearance | powder to crystal |
| Color | White to Gray to Brown |
| pKa | 1.45±0.10(Predicted) |
| Storage Condition | Store at +4°C |
| Refractive Index | 1.577 |
| Use | A selective, potent, and irreversible ErbB2 and EGFR inhibitor. |
| In vitro study | Mubritinib effectively inhibits human epidermal growth factor receptor 2(HER2/erbB2) with an IC50 of 6 nM, compared with other tyrosine kinases such as EGFR, FGFR, PDGFR, Jak1, Src and Blk, the selectivity is more than 4000 times higher. When the concentration of Mubritinib is as low as 0.1 μm, when acting on the cell line BT474 carrying high levels of HER2, it also significantly inhibits the phosphorylation of HER2, resulting in the down-regulation of PI3K-Akt and MAPK pathways. Mubritinib not only has a highly effective anti-proliferation effect when it acts on the tumor cell line BT474 that overexpresses ErbB2, with an IC50 of 5 nM, but also has a significant anti-proliferation effect when it acts on the cell lines that express HER2 every week, when applied to LNCaP, LN-REC4 and T24 cells, the IC50 was 53 nM, 90 nM and 91 nM, respectively. When Mubritinib acts on PC-3 cells with very weak expression of HER2, it has no inhibitory activity, and the IC50 is 4.62 μm. When Mubritinib acts on HT1376 and ACHN cell lines with over-expression of EGFR, it also has no inhibitory activity, IC50>25 μm. |
| In vivo study | Mubritinib significantly inhibited LN-REC4 xenograft tumors, with an experimental/control tumor volume ratio of 26.5 percent. Although Mubritinib did not inhibit UMUC-3 and ACHN cells in vitro (IC50s 1.812 and> 25 μm, respectively), Mubritinib was administered orally at a dose of 10 or 20 mg/kg per day, the growth of UMUC-3 and ACHN xenografts was significantly inhibited, and the tumor volume ratio of experimental group/control group was 22.9 and 26%, respectively, while Herceptin was used to treat UMUC-3 tumors at a dose of 20 mg/kg, no effect on tumor growth. |
Mubritinib - Introduction
Mubritinib (TAK 165) is a potent HER2/ErbB2 inhibitor with an IC50 of 6 nM; it has no inhibitory activity on EGFR, FGFR, PDGFR, JAK1, Src and Blk.
Last Update：2022-10-16 17:24:54
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Product Name: Mubritinib (TAK 165) Visit Supplier Webpage Request for quotation
CAS: 366017-09-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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CAS: 366017-09-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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