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Mubritinib (TAK 165)

Potent and selective ErbB2 inhibitor CAS# 366017-09-6

Mubritinib (TAK 165)

Catalog No. BCC4513----Order now to get a substantial discount!

Product Name & Size Price Stock
Mubritinib (TAK 165): 5mg $23 In Stock
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Chemical structure

Mubritinib (TAK 165)

3D structure

Chemical Properties of Mubritinib (TAK 165)

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.
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.
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.

Biological Activity of Mubritinib (TAK 165)

DescriptionPotent, 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

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Mubritinib (TAK 165) Molarity Calculator

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Preparing Stock Solutions of Mubritinib (TAK 165)

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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Background on Mubritinib (TAK 165)

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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References on Mubritinib (TAK 165)

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).

Description

Mubritinib (TAK-165) is a potent and selective EGFR2/HER2 inhibitor with an IC50 of 6 nM.

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