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| Cas No.: | 366017-09-6 |
| Chemical Name: | (E)-1-(4-(4-((2-(4-(trifluoromethyl)styryl)oxazol-4-yl)methoxy)phenyl)butyl)-1H-1,2,3-triazole |
| Synonyms: | TAK165,TAK-165 |
| SMILES: | FC(C1=CC=C(/C=C/C2=NC(COC3=CC=C(CCCCN4N=NC=C4)C=C3)=CO2)C=C1)(F)F |
| Formula: | C25H23F3N4O2 |
| M.Wt: | 468.47 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | Mubritinib (TAK-165) is a potent and selective EGFR2/HER2 inhibitor with an IC50 of 6 nM. |
| Target: | HER2:6 nM (IC50) |
| In Vivo: | In the xenograft model, treatment with 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]. |
| In Vitro: | 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. TAK-165 inhibits HER2 phosphorylation and its down-stream Akt and MAPK in HER2 strongly expressing cells (BT474 breast cancer cell line). TAK-165 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]. |
| Cell Assay: | Cells are treated with TAK-165 at various concentrations for 72 h. After the incubation period, the cells are counted. The IC50 value is calculated from a dose–response curve generated by least-squares linear regression of the response[1]. |
| Animal Administration: | Mice: UMUC-3 and LN-REC4 cells are implanted with 50% Matrigel solution. After the tumor volume reaches 200–300 mm3 in LN-REC4 and UMUC-3 cells and to 100–200 mm3 in ACHN, the mice are treated orally twice daily for 14 days with vehicle (control) or 10 or 20 mg/kg per day of TAK-165. In the Herceptin study against UMUC-3, treatments consist of a twice weekly intraperitoneal injection of 20 mg/kg Herceptin in PBS for 2 weeks. Tumor growth is assessed by electronic caliper measurement of tumor diameter in two dimensions, and tumor volume is calculated[1]. |
| References: | [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. |