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> Mubritinib [366017-09-6]

Mubritinib [366017-09-6]

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Référence HY-13501-100mg

Conditionnement : 100mg

Marque : MedChemExpress

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Description

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

IC50 & Target[1]

HER2

6 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
A549 IC50
4.27 μM
Compound: Mubritinib
Antiproliferative activity against HER2 weak positive human A549 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Antiproliferative activity against HER2 weak positive human A549 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
[PMID: 35452936]
BEAS-2B CC50
6.42 μM
Compound: Mubritinib
Cytotoxicity against human BEAS-2B cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Cytotoxicity against human BEAS-2B cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
[PMID: 35452936]
HepG2 IC50
3.5 μM
Compound: Mubritinib
Antiproliferative activity against HER2 negative human HepG2 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Antiproliferative activity against HER2 negative human HepG2 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
[PMID: 35452936]
L02 CC50
8.07 μM
Compound: Mubritinib
Cytotoxicity against human L02 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
[PMID: 35452936]
MCF-10A CC50
11.26 μM
Compound: Mubritinib
Cytotoxicity against human MCF-10A cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Cytotoxicity against human MCF-10A cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
[PMID: 35452936]
MCF7 IC50
5.75 μM
Compound: Mubritinib
Antiproliferative activity against HER2 negative human MCF7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Antiproliferative activity against HER2 negative human MCF7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
[PMID: 35452936]
MIA PaCa-2 IC50
51 nM
Compound: Mubritinib
Cytotoxicity against human MIA PaCa-2 cells assessed as inhibition of cell growth incubated for overnight in glucose-containing medium followed by compound addition and measured after 7 days by MTT assay
Cytotoxicity against human MIA PaCa-2 cells assessed as inhibition of cell growth incubated for overnight in glucose-containing medium followed by compound addition and measured after 7 days by MTT assay
[PMID: 35167303]
SK-BR-3 IC50
0.64 μM
Compound: Mubritinib
Antiproliferative activity against human SK-BR-3 cells overexpressing HER2 assessed as reduction in cell viability measured after 24 hrs by MTT assay
Antiproliferative activity against human SK-BR-3 cells overexpressing HER2 assessed as reduction in cell viability measured after 24 hrs by MTT assay
[PMID: 35452936]
In Vitro

Mubritinib (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. Mubritinib inhibits HER2 phosphorylation and its down-stream Akt and MAPK in HER2 strongly expressing cells (BT474 breast cancer cell line). Mubritinib 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].

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

Mubritinib Related Antibodies

Solvant et solubilité
In Vitro: 

DMSO : 50 mg/mL (106.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Pureté et documentation
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