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Varlitinib

Name: Varlitinib
Brand: TargetMol
SKU: T6719
Price: 173 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T6719Cas No. 845272-21-1

Alias ASLAN001, ARRY-334543

Varlitinib (ASLAN001) is a potent, reversible, small molecule pan-EGFR inhibitor with IC50 values of 7 nM for HER1, 2 nM for HER2, and 4 nM for HER4.

Varlitinib

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Purity: 99.7%

Catalog No. T6719Alias ASLAN001, ARRY-334543Cas No. 845272-21-1

Varlitinib (ASLAN001) is a potent, reversible, small molecule pan-EGFR inhibitor with IC50 values of 7 nM for HER1, 2 nM for HER2, and 4 nM for HER4.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$30	In Stock	In Stock
5 mg	$58	In Stock	In Stock
10 mg	$103	In Stock	In Stock
25 mg	$173	In Stock	In Stock
50 mg	Preferential	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$67	In Stock	In Stock

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

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.7%

Appearance:Solid

Color:Orange

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	Varlitinib (ASLAN001) is a potent, reversible, small molecule pan-EGFR inhibitor with IC50 values of 7 nM for HER1, 2 nM for HER2, and 4 nM for HER4.
Targets&IC50	ERB1:7 nM, ErbB2:2 nM, HER4:4 nM
In vitro	In cell-based assays involving tumor cells with over-expression of EGFR (A431) or ErbB-2 (BT474), Varlitinib (ARRY-334543) effectively inhibits substrate phosphorylation and demonstrates high selectivity for EGFR/ErbB-2 without significant activity against a panel of 104 other kinases[2].
In vivo	Varlitinib treatment effectively suppresses tumor growth, achieving complete tumor regression at a dosage of 100 mg/kg administered twice daily. Within five days of treatment, Varlitinib significantly inhibits the phosphorylation of key signaling molecules including HER1-3, RAS/RAF/MEK/MAPK, p70S6K, S6 ribosomal protein, 4EBP1, Cdk-2, Cdc-2, and retinoblastoma. This inhibition is accompanied by a marked decrease in survivin levels and an increase in Caspase 3 cleavage products, indicating enhanced apoptosis. Additionally, in murine xenograft models, Varlitinib (ARRY-334543) shows substantial, dose-dependent tumor growth inhibition in A431-derived tumors when given orally at doses of 25, 50, and 100 mg/kg, twice a day for 21 days.
Synonyms	ASLAN001, ARRY-334543

Chemical Properties

Molecular Weight	466.94
Formula	C₂₂H₁₉ClN₆O₂S
Cas No.	845272-21-1
Smiles	C[C@@H]1COC(Nc2ccc3ncnc(Nc4ccc(OCc5nccs5)c(Cl)c4)c3c2)=N1
Relative Density.	1.51 g/cm3 (Predicted)

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: 31.5 mg/mL (67.46 mM), Sonication and heating to 60℃ are recommended.

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.28 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	2.1416 mL	10.7080 mL	21.4160 mL	107.0801 mL
5 mM	0.4283 mL	2.1416 mL	4.2832 mL	21.4160 mL
10 mM	0.2142 mL	1.0708 mL	2.1416 mL	10.7080 mL
20 mM	0.1071 mL	0.5354 mL	1.0708 mL	5.3540 mL
50 mM	0.0428 mL	0.2142 mL	0.4283 mL	2.1416 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