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Tarloxotinib bromide

Name: Tarloxotinib bromide
Brand: TargetMol
SKU: T13088
Price: 143 USD
Availability: InStock
Rating: 5 (10 reviews)

🥰Excellent

Catalog No. T13088Cas No. 1636180-98-7

Alias TH-4000

Tarloxotinib bromide (TH-4000) is an irreversible inhibitor of EGFR/HER2.

Tarloxotinib bromide

🥰Excellent

Purity: 99.52%

Catalog No. T13088Alias TH-4000Cas No. 1636180-98-7

Tarloxotinib bromide (TH-4000) is an irreversible inhibitor of EGFR/HER2.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$143	In Stock	In Stock
5 mg	$297	In Stock	In Stock
10 mg	$455	In Stock	In Stock
25 mg	$745	In Stock	In Stock
50 mg	$987	In Stock	In Stock
100 mg	$1,380	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$459	In Stock	In Stock

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

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Batch Information

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Purity:99.52%

Appearance:Solid

Color:Yellow

Resource Download

COA LCMS HNMR

Product Introduction

Bioactivity

Description	Tarloxotinib bromide (TH-4000) is an irreversible inhibitor of EGFR/HER2.
In vitro	Tarloxotinib bromide is metabolized efficiently under hypoxia using a panel of human NSCLC cell lines (rate of TKI release 0.4-2.1 nM/hr/106 cells), a process that is inhibited by oxygen (TKI release <0.002 nM/hr/106 cells). Cellular anti-proliferative and receptor phosphorylation assays demonstrate a 14-80 fold reduction of Tarloxotinib bromide activity relative to TKI. Using PC9 tumors, hyperbaric oxygen breathing suppresse release of TKI from Tarloxotinib bromide by >80% (538 vs 99 nM/kg; p<0.01) compared to air breathing controls[1].
In vivo	Tarloxotinib bromide treatment regresses the WT EGFR NSCLC tumor models H125 and H1648, demonstrating Tarloxotinib bromide provides the necessary therapeutic index to inhibit WT EGFR in vivo[2].
Synonyms	TH-4000

Chemical Properties

Molecular Weight	681.77
Formula	C₂₄H₂₄Br₂ClN₉O₃
Cas No.	1636180-98-7
Smiles	[Br-].Cn1cnc(c1C[N+](C)(C)C\C=C\C(=O)Nc1cc2c(Nc3ccc(Cl)c(Br)c3)ncnc2cn1)[N+]([O-])=O
Relative Density.	1.31g/cm3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 33 mg/mL (48.4 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (2.93 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.4668 mL	7.3339 mL	14.6677 mL	73.3385 mL
5 mM	0.2934 mL	1.4668 mL	2.9335 mL	14.6677 mL
10 mM	0.1467 mL	0.7334 mL	1.4668 mL	7.3339 mL
20 mM	0.0733 mL	0.3667 mL	0.7334 mL	3.6669 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

You can also refer to dose conversion for different animals. More Dose Conversion

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