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AZ12601011
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Catalog No. T10426Cas No. 2748337-86-0
Alias AZ-12601011, AZ 12601011
AZ12601011 is an orally active, selective and potent TGFBR1 kinase inhibitor.AZ12601011 inhibits the release of inflammatory factors, interleukin (IL)-1β, IL-6 and tumor necrosis factor-α, and inhibits the growth of breast tumors.AZ12601011 directly binds to TGF-βR1 and blocks downstream Smad3 activation, which can be used to prevent renal fibrosis.
AZ12601011
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Purity: 98.81%
Catalog No. T10426Alias AZ-12601011, AZ 12601011Cas No. 2748337-86-0
AZ12601011 is an orally active, selective and potent TGFBR1 kinase inhibitor.AZ12601011 inhibits the release of inflammatory factors, interleukin (IL)-1β, IL-6 and tumor necrosis factor-α, and inhibits the growth of breast tumors.AZ12601011 directly binds to TGF-βR1 and blocks downstream Smad3 activation, which can be used to prevent renal fibrosis.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $100 | In Stock | In Stock | |
| 5 mg | $247 | In Stock | In Stock | |
| 10 mg | $396 | In Stock | In Stock | |
| 25 mg | $767 | In Stock | In Stock | |
| 50 mg | $1,150 | In Stock | In Stock | |
| 100 mg | $1,590 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $272 | 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:98.81%
Appearance:Solid
Color:Yellow
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | AZ12601011 is an orally active, selective and potent TGFBR1 kinase inhibitor.AZ12601011 inhibits the release of inflammatory factors, interleukin (IL)-1β, IL-6 and tumor necrosis factor-α, and inhibits the growth of breast tumors.AZ12601011 directly binds to TGF-βR1 and blocks downstream Smad3 activation, which can be used to prevent renal fibrosis. |
| Targets&IC50 | ALK4:, TGFBR1:18 nM, TGFBR1:2.9 nM (Kd), TGFβRI:18 nM, TGFβRI:2.9 nM (kd) |
| In vitro | AZ12601011 (0.01-10 μM; for 20 minutes) entirely inhibits phosphorylation of SMAD2 and the activity of ALK4, ALK7, and TGFBR1. It also inhibits 4T1 cell growth in vitro (IC50 = 0.4 μM). [1] Western Blot Analysis shows complete inhibition of SMAD2 phosphorylation in NIH3T3, HaCaT, C2C12, and T47D cells at concentrations of 0.01-10 μM after 20 minutes of incubation. |
| In vivo | AZ12601011 (50mg/kg; oral gavage; twice daily; for 25 days) significantly suppresses tumor growth and metastasis in vivo [1]. Administered to female BALB/c mice (weight >18g) bearing tumors, the compound effectively hinders both tumor development and migration. |
| Synonyms | AZ-12601011, AZ 12601011 |
| Molecular Weight | 313.36 |
| Formula | C19H15N5 |
| Cas No. | 2748337-86-0 |
| Smiles | N=1C=CC2=C(C1)C=CN2C3=NC(=NC4=C3CCC4)C5=NC=CC=C5 |
| Relative Density. | 1.38 g/cm3 at 20℃ (Predicted) |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 4 mg/mL (12.76 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
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Calculator
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, and a total of 10 animals are to be administered, using a formulation of 
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 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 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 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.
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
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