Mubritinib (Synonyms: TAK-165)

Name: Mubritinib
Brand: MedChemExpress
SKU: HY-13501
Rating: 5.0 (7 reviews)

Cat. No.: HY-13501 Purity: 99.90%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 366017-09-6

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 73	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 42	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 224	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 422	In-stock	Estimated Time of Arrival: December 31
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500 mg		Get quote

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Customer Review

Based on 7 publication(s) in Google Scholar

7 Publications Citing Use of MCE Mubritinib

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

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.

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.

Clinical Trial

Molecular Weight

468.47

Formula

C₂₅H₂₃F₃N₄O₂

CAS No.

366017-09-6

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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
10 mM	0.2135 mL	1.0673 mL	2.1346 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.91%

Select Batch:

Data Sheet (271 KB) SDS (392 KB)

COA (244 KB) HNMR (174 KB) LCMS (356 KB)

Handling Instructions (2659 KB)

References

[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]

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

Complete Stock Solution Preparation Table

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

Mubritinib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Mubritinib366017-09-6TAK-165TAK165TAK 165EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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Mubritinib (Synonyms: TAK-165)

Customer Review

Mubritinib Related Antibodies

7 Publications Citing Use of MCE Mubritinib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All EGFR Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Mubritinib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Mubritinib Related Classifications

Keywords:

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