Mubritinib (TAK 165)Potent and selective ErbB2 inhibitor CAS# 366017-09-6 |
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Quality Control & MSDS
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| Cas No. | 366017-09-6 | SDF | Download SDF |
| PubChem ID | 6444692 | Appearance | Powder |
| Formula | C25H23F3N4O2 | M.Wt | 468.47 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | Mubritinib | ||
| Solubility | DMSO : 50 mg/mL (106.73 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble) | ||
| Chemical Name | 4-[[4-[4-(triazol-1-yl)butyl]phenoxy]methyl]-2-[(E)-2-[4-(trifluoromethyl)phenyl]ethenyl]-1,3-oxazole | ||
| SMILES | C1=CC(=CC=C1CCCCN2C=CN=N2)OCC3=COC(=N3)C=CC4=CC=C(C=C4)C(F)(F)F | ||
| Standard InChIKey | ZTFBIUXIQYRUNT-MDWZMJQESA-N | ||
| Standard 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+ | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Potent, irreversible human epithelial growth factor receptor 2 (ErbB2) inhibitor (IC50 = 6 nM) that displays > 4000-fold selectivity over EGFR, FGFR, PDGFR, JAK1 and Src. 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) Dilution Calculator
Mubritinib (TAK 165) Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.1346 mL | 10.673 mL | 21.3461 mL | 42.6922 mL | 53.3652 mL |
| 5 mM | 0.4269 mL | 2.1346 mL | 4.2692 mL | 8.5384 mL | 10.673 mL |
| 10 mM | 0.2135 mL | 1.0673 mL | 2.1346 mL | 4.2692 mL | 5.3365 mL |
| 50 mM | 0.0427 mL | 0.2135 mL | 0.4269 mL | 0.8538 mL | 1.0673 mL |
| 100 mM | 0.0213 mL | 0.1067 mL | 0.2135 mL | 0.4269 mL | 0.5337 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Mubritinib (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM; no activity to EGFR, FGFR, PDGFR, JAK1, Src and Blk.
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Inhibitors of epidermal-growth-factor receptors: a review of clinical research with a focus on non-small-cell lung cancer.[Pubmed:12850190]
Lancet Oncol. 2003 Jul;4(7):397-406.
Despite aggressive surgical and chemotherapeutic interventions, non-small-cell lung cancer (NSCLC) is the leading cause of cancer-related death in men and women with overall cure rates of less than 15%. Recent advances in our understanding of cellular signalling and its critical role in tumorigenesis has led to the development of novel therapies which may offer new hope. In particular, the epidermal growth-factor receptor superfamily is an attractive therapeutic target because it is commonly overexpressed in malignant disease, regulates many vital cellular processes, and seems to be a negative prognostic indicator. Several selective inhibitors of this family of receptors are currently being evaluated in several cancers including NSCLC. In this review we examine current preclinical and clinical evidence on monoclonal antibodies (cetuximab, ABX-EGF, EMD72000, MAb ICR62, h-R3, MDX-447, MDX-H210, trastuzumab, and 2C4), immunoconjugates (Y10, Ua30:2, Mab806), anti-EGF vaccine (YMB2000), and tyrosine kinase inhibitors (gefitinib, erlotinib, CI1033, GW572016, EKB 569, PKI166, PD158780, and TAK 165).
Mubritinib (TAK-165) is a potent and selective EGFR2/HER2 inhibitor with an IC50 of 6 nM.
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