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Pyrotinib dimaleate

Name: Pyrotinib dimaleate
Brand: TargetMol
SKU: T12594
Price: 157 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T12594Cas No. 1397922-61-0

Alias SHR-1258 dimaleate

Pyrotinib dimaleate is a selective EGFR/HER2 dual inhibitor with IC50 values of 13 and 38 nM, respectively, for the treatment of HER2-positive breast cancer.

Pyrotinib dimaleate

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Purity: 99.52%

Catalog No. T12594Alias SHR-1258 dimaleateCas No. 1397922-61-0

Pyrotinib dimaleate is a selective EGFR/HER2 dual inhibitor with IC50 values of 13 and 38 nM, respectively, for the treatment of HER2-positive breast cancer.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$157	In Stock	In Stock
5 mg	$482	In Stock	In Stock
10 mg	$642	In Stock	In Stock
25 mg	$996	In Stock	In Stock
50 mg	$1,370	In Stock	In Stock
100 mg	$1,850	-	In Stock
1 mL x 10 mM (in DMSO)	$652	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

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Batch Information

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Purity:99.52%

Appearance:Solid

Color:Yellow

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COA HPLC HNMR

Product Introduction

Bioactivity

Description	Pyrotinib dimaleate is a selective EGFR/HER2 dual inhibitor with IC50 values of 13 and 38 nM, respectively, for the treatment of HER2-positive breast cancer.
Targets&IC50	EGFR:13 nM, HER2:38 nM
In vitro	METHODS: SK-BR-3 cells were treated with Pyrotinib dimaleate (10nM) + chrysin (20μM) or drug + mimics and drug + si-ZBTB16, and the cells were collected for apoptosis analysis. RESULTS Pyrotinib dimaleate + chrysin treatment led to a significant upregulation of ZBTB16 expression, and this effect was neutralized by knockdown of ZBTB16 by siRNA-ZBTB16; miR-16-5p overexpression or ZBTB16 knockdown correspondingly reduced the apoptosis rate induced by Pyrotinib dimaleate + chrysin treatment. [2]
In vivo	METHODS: Nude mice with tumor xenografts of BT-474 or SK-BR-3 cells were treated with Pyrotinib dimaleate (10 mg/kg, gavage, 21 days), chrysin (50 mg/kg), or their combination, and the effect of miR-16-5p expression level on anti-tumor efficacy was analyzed. RESULTS Combination therapy of pyrotinib dimaleate and chrysin synergistically enhanced autophagy in HER2-positive breast cancer cells by regulating the miR-16-5p/ZBTB16/G6PD axis.[2]
Synonyms	SHR-1258 dimaleate

Chemical Properties

Molecular Weight	815.22
Formula	C₄₀H₃₉ClN₆O₁₁
Cas No.	1397922-61-0
Smiles	OC(=O)\C=C/C(O)=O.OC(=O)\C=C/C(O)=O.CCOc1cc2ncc(C#N)c(Nc3ccc(OCc4ccccn4)c(Cl)c3)c2cc1NC(=O)\C=C\[C@H]1CCCN1C
Relative Density.	no data available

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: 50 mg/mL (61.33 mM), Sonication is recommended.

Ethanol: 40 mg/mL (49.07 mM), Sonication is recommended.

DMSO: 240 mg/mL (294.4 mM), Sonication is recommended.

Solution Preparation Table

Ethanol/H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	1.2267 mL	6.1333 mL	12.2666 mL	61.3331 mL
5 mM	0.2453 mL	1.2267 mL	2.4533 mL	12.2666 mL
10 mM	0.1227 mL	0.6133 mL	1.2267 mL	6.1333 mL
20 mM	0.0613 mL	0.3067 mL	0.6133 mL	3.0667 mL

H2O/DMSO

	1mg	5mg	10mg	50mg
50 mM	0.0245 mL	0.1227 mL	0.2453 mL	1.2267 mL

DMSO

	1mg	5mg	10mg	50mg
100 mM	0.0123 mL	0.0613 mL	0.1227 mL	0.6133 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc