| Name | AZ12601011 |
| 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. |
| 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. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 4 mg/mL (12.76 mM), Sonication is recommended.
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| Keywords | TGFβR1 | TGF-β/Smad | TGFβ | TGFBR1 | TGFbeta/Smad | TGF-beta | TGFbeta | TGF-b/Smad | TGFb | Smad | AZ12601011 | ALK4 |
| Inhibitors Related | Alectinib | Trimethylamine N-oxide | Melamine | SB-431542 | Hydrochlorothiazide | Crizotinib | Brigatinib | Pirfenidone | A 83-01 | Cetrimonium bromide | Galunisertib | Alantolactone |
| Related Compound Libraries | Anti-Lung Cancer Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Angiogenesis related Compound Library | Inhibitor Library | Stem Cell Differentiation Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | TGF-beta/Smad Compound Library |