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AZ12601011
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
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 | Availability | Quantity |
|---|---|---|---|
| 1 mg | $100 | In Stock | |
| 5 mg | $247 | In Stock | |
| 10 mg | $396 | In Stock | |
| 25 mg | $767 | In Stock | |
| 50 mg | $1,150 | In Stock | |
| 100 mg | $1,590 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $272 | In Stock |
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Purity:98.81%
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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.Product Introduction
Bioactivity
Chemical Properties
| 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:, TGFBR1:2.9 nM (Kd), TGFBR1:18 nM, 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. |
| Alias | AZ-12601011, AZ 12601011 |
| Molecular Weight | 313.36 |
| Formula | C19H15N5 |
| Cas No. | 2748337-86-0 |
Storage & Solubility Information
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
| Solubility Information | DMSO: 4 mg/mL (12.76 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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(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 DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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