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Chemical Structure| 366017-09-6 Chemical Structure| 366017-09-6

Structure of Mubritinib
CAS No.: 366017-09-6

Chemical Structure| 366017-09-6

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

Synonyms: TAK-165

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Product Details of Mubritinib

CAS No. :366017-09-6
Formula : C25H23F3N4O2
M.W : 468.47
SMILES Code : FC(F)(C1=CC=C(/C=C/C2=NC(COC3=CC=C(C=C3)CCCCN4C=CN=N4)=CO2)C=C1)F
Synonyms :
TAK-165
MDL No. :MFCD09954135
InChI Key :ZTFBIUXIQYRUNT-MDWZMJQESA-N
Pubchem ID :6444692

Safety of Mubritinib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H320-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of Mubritinib

RTK

Isoform Comparison

Biological Activity

Target
  • HER2

    HER2/ErbB2, IC50:6.0 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Asthmatic human airway epithelial cells (Asthmatic HAECs) 100 nM 16 h Inhibition of ErbB2 phosphorylation had minimal effect on wound closure and CCND1 expression in asthmatic HAECs, indicating lower ErbB2 activity in these cells. J Allergy Clin Immunol. 2019 Jun;143(6):2075-2085.e10.
Healthy human airway epithelial cells (HC HAECs) 100 nM 16 h Inhibition of ErbB2 phosphorylation significantly reduced wound closure and CCND1 expression in healthy HAECs, but had less impact on asthmatic HAECs. J Allergy Clin Immunol. 2019 Jun;143(6):2075-2085.e10.
BTSC147 500 nM 24 h Measure basal oxygen consumption rate (OCR), results showed Mubritinib significantly reduced basal mitochondrial respiration in BTSC147 EMBO Mol Med. 2025 Mar;17(3):469-503.
BTSC73 100 nM 24 h Measure basal oxygen consumption rate (OCR), results showed Mubritinib significantly reduced basal mitochondrial respiration in BTSC73 EMBO Mol Med. 2025 Mar;17(3):469-503.
BTSC53 20 nM 24 h Measure basal oxygen consumption rate (OCR), results showed Mubritinib significantly reduced basal mitochondrial respiration in BTSC53 EMBO Mol Med. 2025 Mar;17(3):469-503.
OCI-AML3 cells 125 nM 24 h TAK-165 in combination with AC220 significantly reduced the viability of OCI-AML3 cells Cell Death Dis. 2018 Jan 26;9(2):138.
HEL cells 125 nM 24 h TAK-165 in combination with AC220 significantly reduced the viability of HEL cells Cell Death Dis. 2018 Jan 26;9(2):138.
Sum159 cells 125 nM 24 h TAK-165 in combination with AC220 significantly reduced the viability of Sum159 cells Cell Death Dis. 2018 Jan 26;9(2):138.
ES-2 cells 125 nM 24 h TAK-165 in combination with AC220 significantly reduced the viability of ES-2 cells Cell Death Dis. 2018 Jan 26;9(2):138.
SNU-16R cells 1 µM 72 h To evaluate the effect of Mubritinib on the growth of SNU-16R cells, the results showed that SNU-16R cells were sensitive to Mubritinib Gastric Cancer. 2016 Jan;19(1):53-62.
BT474 cells 10 µM 24 h Selective inhibition of HER2 significantly reduced the mitochondrial metabolic rate of BT474 cells, but the effect was less pronounced than in SK-BR3 cells. Oncogenesis. 2018 Aug 24;7(8):64.
SK-BR3 cells 10 µM 24 h Selective inhibition of HER2 significantly reduced the mitochondrial metabolic rate of SK-BR3 cells by ~40%. Oncogenesis. 2018 Aug 24;7(8):64.
BC1 cells 15 nM 72 h To investigate the effect of Mubritinib on the cell cycle of PEL cells, Mubritinib reduced S and G2 populations and increased the sub-G1 population in BC1 cells. Oncotarget. 2020 Nov 17;11(46):4224-4242.
BCBL1 cells 15 nM 72 h To investigate the effect of Mubritinib on the cell cycle of PEL cells, Mubritinib reduced S and G2 populations and increased the sub-G1 population in BCBL1 cells. Oncotarget. 2020 Nov 17;11(46):4224-4242.
BC3 cells 10 µM 72 h To screen for drugs that selectively inhibit the growth of KSHV+ PEL cells, Mubritinib showed growth inhibition in BC3 cells. Oncotarget. 2020 Nov 17;11(46):4224-4242.
Rat brain endothelial cells (RBECs) 1 µM 6 h To evaluate the protective effect of Mubritinib on the blood-spinal cord barrier function under oxygen-glucose deprivation and reoxygenation stress, results showed that Mubritinib significantly increased TEER and reduced Na-F permeability. Neurotherapeutics. 2022 Oct;19(6):1976-1991.
hCMEC/D3 cells 10 µM 24 h To evaluate the protective effect of Mubritinib on hCMEC/D3 cells under oxidative stress, results showed that Mubritinib protected cells from H2O2-induced oxidative stress damage. Neurotherapeutics. 2022 Oct;19(6):1976-1991.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice GBM model Intraperitoneal injection 6 mg/kg 3 times per week for 40 days Evaluate the effect of Mubritinib on GBM tumor growth, results showed Mubritinib significantly delayed tumor growth and extended animal survival EMBO Mol Med. 2025 Mar;17(3):469-503.
Mice PEL mouse models Oral 25 mg/kg Once daily for 34 days To evaluate the inhibitory effect of Mubritinib on PEL cell growth in vivo, Mubritinib significantly slowed tumor growth in BCBL1 and BC1 mice. Oncotarget. 2020 Nov 17;11(46):4224-4242.
Mice Spinal cord injury model Intraperitoneal injection 1 mg/kg Once daily for one day To evaluate the protective effect of Mubritinib on the blood-spinal cord barrier after spinal cord injury, results showed that Mubritinib significantly reduced IgG and Alb leakage. Neurotherapeutics. 2022 Oct;19(6):1976-1991.

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00034281 Breast Neoplasm|Pancreatic Neo... More >>plasm|Lung Neoplasm|Ovarian Neoplasm|Renal Neoplasm Less << PHASE1 COMPLETED 2025-09-03 Arizona Cancer Center, Scottsd... More >>ale, Arizona, 85258, United States|The Institute for Drug Development, San Antonio, Texas, 78229, United States|Brooke Army Medical Center/Drug Development Unit, San Antonio, Texas, 78234, United States|South Texas VA, Audie Murphy Division, San Antonio, Texas, 78284, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.13mL

0.43mL

0.21mL

10.67mL

2.13mL

1.07mL

21.35mL

4.27mL

2.13mL

 

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