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Mubritinib

Catalog No. T6124   CAS 366017-09-6
Synonyms: TAK-165

Mubritinib (TAK-165) (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM.

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Mubritinib Chemical Structure
Mubritinib, CAS 366017-09-6
Pack Size Availability Price/USD Quantity
5 mg In stock $ 32.00
10 mg In stock $ 52.00
25 mg In stock $ 105.00
50 mg In stock $ 183.00
100 mg In stock $ 349.00
1 mL * 10 mM (in DMSO) In stock $ 50.00
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Purity: 99.87%
Purity: 99.85%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Mubritinib (TAK-165) (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM.
Targets&IC50 HER2/ErbB2:6.0 nM
In vitro Mubritinib displays > 4000-fold selectivity over other tyrosine kinases, such as EGFR, FGFR, PDGFR, Jak1, Src and Blk. Mubritinib even at low concentration of 0.1 μM significantly blocks HER2 phosphorylation, leading to the downregulation of PI3K-Akt and MAPK pathway in cell line BT474 with high level of HER2. Mubritinib not only exhibits highly potent antiproliferative effect in ErbB2-overexpressing cancer cell line BT474 with an IC50 of 5 nM, but also displays marked antiproliferative effects in cell lines with HER2 expressed weakly with IC50 of 53 nM, 90 nM and 91 nM for LNCaP, LN-REC4 and T24, respectively. Mubritinib displays no inhibitory activities against PC-3 cells with HER2 expressed very faintly with IC50 of 4.62 μM, as well as EGFR-overexpressing HT1376 and ACHN cell lines with IC50 of >25 μM. [1]
In vivo Mubritinib significantly inhibits LN-REC4 xenograft with treatment/control tumor volume ratio of 26.5%. Although ineffective to inhibit the growth of UMUC-3 and ACHN cells in vitro (IC50s of 1.812 and >25 μM, respectively), oral administration of Mubritinib (10 or 20 mg/kg per day) significantly inhibits the growth of UMUC-3 and ACHN xenografts with treatment/control tumor volume ratio of 22.9% and 26%, respectively, as compared with Herceptin (20 mg/kg) which is ineffective to UMUC-3 tumor growth. [1]
Kinase Assay Inhibition of HER2/erbB2 tyrosine kinase activity: BT-474 cells are seeded on 24-well plates and cultured overnight. Mubritinib is then added at various concentrations. After incubation for 2 hours, the cells are harvested directly into sodium dodecyl sulfate (SDS)-sample buffer (200 μL). Aliquots containing equal amounts of total cell extract are run on 7.5% to 15% gradient SDS–polyacrylamide gel electrophoresis (PAGE). Following electrophoresis, proteins are transferred onto a polyvinylidene fluoride (PVDF) membrane, for western blot analysis using a relevant primary antibody. Detection of protein is accomplished by an enhanced chemiluminescent (ECL) detection method. The extent of tyrosine phosphorylation of HER2/erbB2 is measured by the LAS-1000 plus lumino-image analyser. The concentration of Mubritinib that inhibits HER2/erbB2 phosphorylation by 50% (IC50) is calculated from a dose–response curve generated by least-squares linear regression of the response using SAS software.
Cell Research Cells are seeded into 6-well plates and cultured overnight. Mubritinib is then added at various concentrations, and the cells are treated continuously for 72 hours. After the incubation period, cells are counted for the measurement of antiproliferative activity.(Only for Reference)
Synonyms TAK-165
Molecular Weight 468.47
Formula C25H23F3N4O2
CAS No. 366017-09-6

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 35.1 mg/mL (75 mM)

TargetMolReferences and Literature

1. Nagasawa J, et al. Int J Urol, 2006, 13(5), 587-592.

TargetMolCitations

1. Hong J H, Yong C H, Heng H L, et al.Integrative multiomics enhancer activity profiling identifies therapeutic vulnerabilities in cholangiocarcinoma of different etiologies.Gut.2023

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Tyrosine Kinase Inhibitor Library Highly Selective Inhibitor Library Bioactive Compounds Library Max Anti-Colorectal Cancer Compound Library Osteogenesis Compound Library Reprogramming Compound Library Anti-Pancreatic Cancer Compound Library

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Keywords

Mubritinib 366017-09-6 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors EGFR FGFR JAK PDGFR Epidermal growth factor receptor inhibit Inhibitor TAK-165 HER1 ErbB-1 TAK165 TAK 165 inhibitor

 

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