Mubritinib (Synonyms: TAK-165)

Name: Mubritinib
Brand: MedChemExpress
SKU: HY-13501
Rating: 5.0 (8 reviews)

製品番号: HY-13501 純度: 99.76%: Data Sheet SDS COA 取扱説明書
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Technical Support

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

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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Mubritinib 構造式

CAS 番号 : 366017-09-6

容量	価格（税別）	在庫状況	数量

>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 43	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 43	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$42	在庫あり	Estimated Time of Arrival: December 31
10 mg	$66	在庫あり	Estimated Time of Arrival: December 31
25 mg	$150	在庫あり	Estimated Time of Arrival: December 31
50 mg	$224	在庫あり	Estimated Time of Arrival: December 31
100 mg	$422	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 8 publication(s) in Google Scholar

顧客検証

EGFR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

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

生物活性
プロトコル
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

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 3 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]
A549	IC₅₀	4.27 3 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]
A549	IC₅₀	4.27 3 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 3 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]
BEAS-2B	CC₅₀	6.42 3 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]
BEAS-2B	CC₅₀	6.42 3 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 3 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]
HepG2	IC₅₀	3.5 3 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]
HepG2	IC₅₀	3.5 3 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 3 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]
L02	CC₅₀	8.07 3 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]
MIA PaCa-2	IC₅₀	51 1 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]
MCF-10A	CC₅₀	11.26 3 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]
L02	CC₅₀	8.07 3 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 3 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 3 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]
MCF7	IC₅₀	5.75 3 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 1 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]
MCF-10A	CC₅₀	11.26 3 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 3 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]
SK-BR-3	IC₅₀	0.64 3 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]
SK-BR-3	IC₅₀	0.64 3 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]
MIA PaCa-2	IC₅₀	51 1 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 3 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]

体外実験

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.

体内実験

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.

臨床実験

分子量

468.47

分子式

C₂₅H₂₃F₃N₄O₂

CAS 番号

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

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)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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.

純度とドキュメンテーション

純度: 99.91%

Select Batch:

データシート (271 KB) SDS (392 KB)

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

取扱説明書 (2659 KB)

参考文献

[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]

細胞実験 ^[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) はこれらの方法の精度を確認していません。こちらは参照専用です。
動物実験 ^[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) はこれらの方法の精度を確認していません。こちらは参照専用です。
参考文献	[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

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

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)

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Molarity Calculator

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Complete Stock Solution Preparation Table

Mubritinib Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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Mubritinib (Synonyms: TAK-165)

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Mubritinib 関連抗体

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

EGFR アイソフォーム固有の製品をすべて表示:

生物活性

プロトコル

純度とドキュメンテーション

参考文献

カスタマーレビュー

Mubritinib 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Mubritinib Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

カスタマーレビュー

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