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AV-412

Name: AV-412
Brand: TargetMol
SKU: T10419
Price: 37 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T10419Cas No. 451493-31-5

Alias MP412

AV-412 (MP412) is an EGFR inhibitor for EGFR, EGFR T790M, EGFR L858R, EGFR L858R/T790M, and ErbB2, with IC50 values of 0.75, 0.79, 0.5, 2.3, and 19 nM, respectively.

AV-412

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Purity: 99.92%

Catalog No. T10419Alias MP412Cas No. 451493-31-5

AV-412 (MP412) is an EGFR inhibitor for EGFR, EGFR T790M, EGFR L858R, EGFR L858R/T790M, and ErbB2, with IC50 values of 0.75, 0.79, 0.5, 2.3, and 19 nM, respectively.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$37	In Stock	In Stock
2 mg	$53	In Stock	In Stock
5 mg	$87	In Stock	In Stock
10 mg	$147	In Stock	In Stock
25 mg	$267	In Stock	In Stock
50 mg	$447	In Stock	In Stock
100 mg	$646	-	In Stock
1 mL x 10 mM (in DMSO)	$138	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:99.92%

Appearance:Solid

Color:White to Yellow

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	AV-412 (MP412) is an EGFR inhibitor for EGFR, EGFR T790M, EGFR L858R, EGFR L858R/T790M, and ErbB2, with IC50 values of 0.75, 0.79, 0.5, 2.3, and 19 nM, respectively.
Targets&IC50	EGFR (T790M):0.79 nM, EGFR:0.75 nM, EGFR (L858R):0.5 nM, ErbB2:19 nM, EGFR (L858R/T790M):2.3 nM
In vitro	In cells, MP-412 inhibited autophosphorylation of EGFR and ErbB2 with IC(50) of 43 and 282 nM, respectively. It also inhibited epidermal growth factor (EGF)-dependent cell proliferation with an IC(50) of 100 nM. Moreover, MP-412 abrogated EGFR signaling in the gefitinib-resistant H1975 cell line, which harbors a double mutation of L858R and T790M in EGFR.
In vivo	In animal studies using cancer xenograft models, MP-412 (30 mg/kg) demonstrated complete inhibition of tumor growth in A431 and BT-474 cell lines, which overexpress EGFR and ErbB2, respectively. MP-412 suppressed EGFR and ErbB2 autophosphorylation at doses corresponding to its antitumor efficacy. Various dosing schedules showed significant effects with daily and every-other-day schedules, but not with a once-weekly schedule, suggesting frequent dosing is preferable. Additionally, MP-412 exhibited significant antitumor effects on the ErbB2-overexpressing KPL-4 breast cancer cell line, which is resistant to gefitinib. These studies indicate MP-412's potential as a therapeutic for cancers expressing EGFR and ErbB2, especially those resistant to first-generation small-molecule inhibitors.
Synonyms	MP412

Chemical Properties

Molecular Weight	851.41
Formula	C₄₁H₄₄ClFN₆O₇S₂
Cas No.	451493-31-5
Smiles	Cc1ccc(cc1)S(O)(=O)=O.Cc1ccc(cc1)S(O)(=O)=O.CN1CCN(CC1)C(C)(C)C#Cc1cc2ncnc(Nc3ccc(F)c(Cl)c3)c2cc1NC(=O)C=C
Relative Density.	no data available

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 135 mg/mL (158.56 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (2.35 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	1.1745 mL	5.8726 mL	11.7452 mL	58.7261 mL
5 mM	0.2349 mL	1.1745 mL	2.3490 mL	11.7452 mL
10 mM	0.1175 mL	0.5873 mL	1.1745 mL	5.8726 mL
20 mM	0.0587 mL	0.2936 mL	0.5873 mL	2.9363 mL
50 mM	0.0235 mL	0.1175 mL	0.2349 mL	1.1745 mL
100 mM	0.0117 mL	0.0587 mL	0.1175 mL	0.5873 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