Mubritinib (TAK 165)

For research use only.

Catalog No.S2216

26 publications

Mubritinib (TAK 165) Chemical Structure

CAS No. 366017-09-6

Mubritinib (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM in BT-474 cell; no activity to EGFR, FGFR, PDGFR, JAK1, Src and Blk in BT-474 cell line. Phase 1.

Selleck's Mubritinib (TAK 165) has been cited by 26 publications

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Biological Activity

Description Mubritinib (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM in BT-474 cell; no activity to EGFR, FGFR, PDGFR, JAK1, Src and Blk in BT-474 cell line. Phase 1.
HER2/ErbB2 [1]
(BT-474 cells)
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]

Methods Test Index PMID
Western blot
pERK / ERK / pAKT / AKT / p-STAT3 / STAT3 / pHER2 / HER2 ; 

PubMed: 25407459     

Immunoblot analysis of protein phosphorylation status in parental SNU-16 cells and SNU-16 cells resistant to AZD4547 (ADZR) treated for 2 h with the indicated concentrations of mubritinib. BGJR SNU-16 cell line resistant to BGJ398, ERK extracellular-signal-regulated kinase, PDR SNU-16 cell line resistant to PD173074, pERK phosphorylated extracellular-signal-regulated kinase, pHER2 phosphorylated HER2, pSTAT3 phosphorylated signal transducer and activator of transcription 3, STAT3 signal transducer and activator of transcription 3

c-myc / p21 / p27 ; 

PubMed: 27074819     

A western blot analysis of c-myc, p21 and p27 protein in HL60 and NB4 cells. The cells were treated with the indicated concentrations of TAK165 for 3 days.

25407459 27074819
Growth inhibition assay
Cell viability; 

PubMed: 25407459     

Cell viability assay of a parental cell line and resistant cell lines following 72 h of incubation with increasing concentrations of mubritinib. Each data point represents the mean of two independent triplicate measurements, and error bars indicate the standard deviation.

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:[1]
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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:[1]
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  • Cell lines: BT474, HT1376, UMUC-3, T24, ACHN, DU-145, PC-3, LN-REC4, and LNCaP cells
  • Concentrations: Dissolved in DMSO, final concentrations ~50 mM
  • Incubation Time: 72 hours
  • Method: 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)
Animal Research:[1]
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  • Animal Models: Athymic nude mice (BALB/c nu/nμ) and SCID mice (C.B.-17 Scid/Scid) are implanted subcutaneously with UMUC-3, LN-REC4 or ACHN cells
  • Dosages: 10 or 20 mg/kg/day
  • Administration: Orally twice daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 13 mg/mL (27.74 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.
5 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 468.47


CAS No. 366017-09-6
Storage powder
in solvent
Synonyms N/A
Smiles C1=CC(=CC=C1CCCCN2C=CN=N2)OCC3=COC(=N3)C=CC4=CC=C(C=C4)C(F)(F)F

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00034281 Completed Drug: TAK-165 Breast Neoplasm|Pancreatic Neoplasm|Lung Neoplasm|Ovarian Neoplasm|Renal Neoplasm Takeda June 2002 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID