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Tarloxotinib bromide

🥰Excellent
Catalog No. T13088Cas No. 1636180-98-7
Alias TH-4000

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

Tarloxotinib bromide

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 SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$143In StockIn Stock
5 mg$297In StockIn Stock
10 mg$455In StockIn Stock
25 mg$745In StockIn Stock
50 mg$987In StockIn Stock
100 mg$1,380In StockIn Stock
1 mL x 10 mM (in DMSO)$459In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.52%
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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].
SynonymsTH-4000
Chemical Properties
Molecular Weight681.77
FormulaC24H24Br2ClN9O3
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
StoragePowder: -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
1mg5mg10mg50mg
1 mM1.4668 mL7.3339 mL14.6677 mL73.3385 mL
5 mM0.2934 mL1.4668 mL2.9335 mL14.6677 mL
10 mM0.1467 mL0.7334 mL1.4668 mL7.3339 mL
20 mM0.0733 mL0.3667 mL0.7334 mL3.6669 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 mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.
1 Enter information below:
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2 Enter the in vivo formulation:
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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

Keywords

TH4000TH 4000Tarloxotinib bromideTarloxotinib BromideTarloxotinibInhibitorinhibitHER2HER1ErbB-1Epidermal growth factor receptorEGFR/HER2EGFR
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