Referencia número: HY-13501

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Mubritinib

(Synonyms: TAK-165)

8 Cited Publications

Revisión del cliente

Based on 8 publication(s) in Google Scholar

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

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Pureza: 99.86%
No. CAS: 366017-09-6
Fòrmula: C₂₅H₂₃F₃N₄O₂
Peso molecular:468.47

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Mubritinib Chemical Structure

No. CAS: 366017-09-6

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (8)
Solvente y solubilidad
- In Vitro
- In Vivo
Protocolo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

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

IC₅₀ & Target^[1]

HER2

6 nM (IC₅₀)

Ver todos los productos específicos de isoformas EGFR :

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.

In Vivo

In the xenograft model, treatment with Mubritinib (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].

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

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 366017-09-6
Appearance Solid
Peso molecular 468.47
Fòrmula C₂₅H₂₃F₃N₄O₂
Color Off-white to light yellow
SMILES

FC(C1=CC=C(/C=C/C2=NC(COC3=CC=C(CCCCN4N=NC=C4)C=C3)=CO2)C=C1)(F)F
Synonyms

TAK-165
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (8)

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Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Pharmacol Res

Time-dependent proteomics and drug response in expanding cancer cells. [Abstract]

2024 May 9:204:107208. PMID: 38729587
Cell Death Dis

Nuclear ErbB2 represses DEPTOR transcription to inhibit autophagy in breast cancer cells. [Abstract]

2021 Apr 14;12(4):397. PMID: 33854045
Microbiol Spectr

Identification of In Vitro Inhibitors of Monkeypox Replication. [Abstract]

2023 Aug 17;11(4):e0474522. PMID: 37278625
bioRxiv

2025 May 31.
bioRxiv

2024 Jan 16.
bioRxiv

Antivirals against monkeypox infections. [Abstract]

2023 Apr 19:2023.04.19.537483. PMID: 37131608
Oncotarget

MEK is a promising target in the basal subtype of bladder cancer. [Abstract]

2020 Nov 3;11(44):3921-3932. PMID: 33216841

Solvente y solubilidad

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocolo

Cell Assay^[1]

Cells are treated with Mubritinib at various concentrations (5 nM-25 μM) 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].

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

Animal Administration^[1]

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 Mubritinib^[1].

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (271 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Nagasawa J, et al. Novel HER2 selective tyrosine kinase inhibitor, TAK-165, inhibits bladder, kidney and androgen-independent prostate cancer in vitro and in vivo. Int J Urol. 2006 May;13(5):587-92. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1346 mL	10.6730 mL	21.3461 mL	53.3652 mL
	5 mM	0.4269 mL	2.1346 mL	4.2692 mL	10.6730 mL
	10 mM	0.2135 mL	1.0673 mL	2.1346 mL	5.3365 mL
	15 mM	0.1423 mL	0.7115 mL	1.4231 mL	3.5577 mL
	20 mM	0.1067 mL	0.5337 mL	1.0673 mL	2.6683 mL
	25 mM	0.0854 mL	0.4269 mL	0.8538 mL	2.1346 mL
	30 mM	0.0712 mL	0.3558 mL	0.7115 mL	1.7788 mL
	40 mM	0.0534 mL	0.2668 mL	0.5337 mL	1.3341 mL
	50 mM	0.0427 mL	0.2135 mL	0.4269 mL	1.0673 mL
	60 mM	0.0356 mL	0.1779 mL	0.3558 mL	0.8894 mL
	80 mM	0.0267 mL	0.1334 mL	0.2668 mL	0.6671 mL
	100 mM	0.0213 mL	0.1067 mL	0.2135 mL	0.5337 mL

Keywords

Mubritinib

8 Cited Publications

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Mubritinib

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Publications Citing Use of MedChemExpress (MCE) Mubritinib

Ver todos los productos específicos de isoformas EGFR

Actividad biológica

Chemical Information

Publications (8)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Mubritinib Related Classifications

HY-13501 Related Classifications