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CAS RN: 366017-09-6 | Product Number: M3058
Mubritinib
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Purity: >98.0%(HPLC)
Synonyms:
- (E)-4-[[4-[4-(1H-1,2,3-Triazol-1-yl)butyl]phenoxy]methyl]-2-[4-(trifluoromethyl)styryl]oxazole
- TAK 165
Product Documents:
| Size | Unit Price | Belgium | Japan* |
|---|---|---|---|
| 25MG |
€182.00
|
Contact Us | 3 |
| 100MG |
€603.00
|
Contact Us | 5 |
*Stock available in Belgium will be delivered in 1 to 3 days
*Stock available in Japan will be delivered in 1 to 2 weeks (excludes regulated items and dry ice shipments).
| Product Number | M3058 |
Purity / Analysis Method 
|
>98.0%(HPLC) |
| Molecular Formula / Molecular Weight | C__2__5H__2__3F__3N__4O__2 = 468.48 |
| Physical State (20 deg.C) | Solid |
| Storage Temperature
|
Refrigerated (0-10°C) |
| Condition to Avoid | Heat Sensitive |
| CAS RN | 366017-09-6 |
| Reaxys Registry Number | 13498857 |
| PubChem Substance ID | 354335238 |
| MDL Number | MFCD09954135 |
Specifications
| Appearance | White to Gray to Brown powder to crystal |
| Purity(HPLC) | min. 98.0 area% |
| Melting point | 158.0 to 162.0 °C |
| NMR | confirm to structure |
Properties (reference)
| Melting Point | 160 °C |
GHS
Related Laws:
Transport Information:
| HS Number | 2934999090 |
Application
ヒト上皮成長因子受容体2 (HER2) チロシンキナーゼ阻害剤，ムブリチニブ
Small-molecule protein kinase inhibitors are widely used to elucidate cellular signaling pathways. Mubritinib (TAK 165) is a selective inhibitor of the human epidermal growth factor receptor 2 (HER2) tyrosine kinase. Reportedly, mubritinib specifically inhibits HER2 tyrosine kinase IC50 6 nmol/L and do not inhibit other types of tyrosine kinase up to 25,000 nmol/L.1) Several reports suggest HER2 expression in bladder cancer, renal cell carcinoma (RCC) and androgen-independent prostate cancer. However, the clinical development program for mubritinib as an anti-cancer drug was discontinued. (The product is for research purpose only.)
References
- 1)Novel HER2 selective tyrosine kinase inhibitor, TAK-165, inhibits bladder, kidney and androgen-independent prostate cancer in vitro and in vivo
- 2)Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity
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