1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. EGFR
  3. Mubritinib

Mubritinib (Synonyms: TAK-165)

Cat. No.: HY-13501 Purity: 99.97%
Handling Instructions

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

For research use only. We do not sell to patients.

Mubritinib Chemical Structure

Mubritinib Chemical Structure

CAS No. : 366017-09-6

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10 mM * 1 mL in DMSO USD 66 In-stock
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Based on 1 publication(s) in Google Scholar

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

IC50 & Target[1]


6 nM (IC50)

In Vitro

TAK-165 specifically inhibits HER2 tyrosine kinase with an IC50 6 nM and does not inhibit other types tyrosine kinase up to 25 000 nM. TAK-165 inhibits HER2 phosphorylation and its down-stream Akt and MAPK in HER2 strongly expressing cells (BT474 breast cancer cell line). TAK-165 sensitivity depends on HER2 levels of each cell line. Especially, BT474 cells which over-express HER2 strongly is highly sensitive (IC50=0.005 µM) and PC-3 cells which express HER2 very weakly is less sensitive (IC50=4.62 µM). But, HT1376 and ACHN cells that over-expressed EGFR showed high IC50 (IC50>25 µM)[1].

In Vivo

In the xenograft model, treatment with TAK-165 significantly inhibits growth of UMUC-3, ACHN, and LN-REC4. The antitumor effect after 14 days treatment are 22.9%, 26.0%, and 26.5% in UMUC3, ACHN and LN-REC4, respectively[1].

Clinical Trial
Molecular Weight









Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (106.73 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1346 mL 10.6730 mL 21.3461 mL
5 mM 0.4269 mL 2.1346 mL 4.2692 mL
10 mM 0.2135 mL 1.0673 mL 2.1346 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (5.34 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution

*All of the co-solvents are provided by MCE.
Cell Assay

Cells are treated with TAK-165 at various concentrations for 72 h. After the incubation period, the cells are counted. The IC50 value is calculated from a dose–response curve generated by least-squares linear regression of the response[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration

Mice: UMUC-3 and LN-REC4 cells are implanted with 50% Matrigel solution. After the tumor volume reaches 200–300 mm3 in LN-REC4 and UMUC-3 cells and to 100–200 mm3 in ACHN, the mice are treated orally twice daily for 14 days with vehicle (control) or 10 or 20 mg/kg per day of TAK-165. In the Herceptin study against UMUC-3, treatments consist of a twice weekly intraperitoneal injection of 20 mg/kg Herceptin in PBS for 2 weeks. Tumor growth is assessed by electronic caliper measurement of tumor diameter in two dimensions, and tumor volume is calculated[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


Purity: 99.97%

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MubritinibTAK-165TAK165TAK 165EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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