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AZ 12799734

Name: AZ 12799734
Brand: TargetMol
SKU: T35896
Price: 40 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T35896Cas No. 1117684-36-2

Alias AZ12799734

AZ 12799734 is an orally active, selective and potent dual inhibitor of TGFBR1 and ALK5 with inhibitory effects on BMP and TGFβ for the study of tumours.

AZ 12799734

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Purity: 98.23%

Catalog No. T35896Alias AZ12799734Cas No. 1117684-36-2

AZ 12799734 is an orally active, selective and potent dual inhibitor of TGFBR1 and ALK5 with inhibitory effects on BMP and TGFβ for the study of tumours.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$40	In Stock	In Stock
5 mg	$93	In Stock	In Stock
10 mg	$148	In Stock	In Stock
25 mg	$295	In Stock	In Stock
50 mg	$483	In Stock	In Stock
100 mg	$653	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$98	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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Purity:98.23%

Appearance:Solid

Color:White

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COA HPLC HNMR

Product Introduction

Bioactivity

Description	AZ 12799734 is an orally active, selective and potent dual inhibitor of TGFBR1 and ALK5 with inhibitory effects on BMP and TGFβ for the study of tumours.
Targets&IC50	TGFβRI:47 nM, ALK1:7.1 μM (Kd), ACVR1:6.2 μM (Kd), ALK6:0.017 μM (Kd), ALK5:0.74 μM (Kd), BMPR1A:40 μM (Kd), ALK4:1 μM (Kd)
In vitro	Inhibiting ligand-activated SMAD3/4 transcription, AZ12799734[2]. AZ12799734 (10 nM; 24 h) inhibits phosphorylation of both SMAD1 and SMAD2[2]. AZ12799734 (500 nM; 36 h) inhibits TGFβ-induced migration in HaCaT epithelial cells[2].
In vivo	Inducing histopathologic heart valve lesions in rats, AZ12799734 is administered orally at doses ranging from 0 to 400 mg/kg/day for 3-7 days[1]. At a single oral dose of 50 mg/kg, AZ12799734 shows total and free pharmacokinetic (PK) levels in nude mice over time, exceeding the in vitro IC50 of 0.01885 μM[2].
Synonyms	AZ12799734

Chemical Properties

Molecular Weight	370.43
Formula	C₁₈H₁₈N₄O₃S
Cas No.	1117684-36-2
Smiles	O(C=1C=C(NC2=CC=C(S(N)(=O)=O)C=C2)N=CC1)C3=C(C)N=C(C)C=C3

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 80 mg/mL (215.97 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.6996 mL	13.4978 mL	26.9957 mL	134.9783 mL
5 mM	0.5399 mL	2.6996 mL	5.3991 mL	26.9957 mL
10 mM	0.2700 mL	1.3498 mL	2.6996 mL	13.4978 mL
20 mM	0.1350 mL	0.6749 mL	1.3498 mL	6.7489 mL
50 mM	0.0540 mL	0.2700 mL	0.5399 mL	2.6996 mL
100 mM	0.0270 mL	0.1350 mL	0.2700 mL	1.3498 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