For research use only. Not for therapeutic Use.
AZ12601011(CAT: I045994) is an orally active and highly selective TGFBR1 kinase inhibitor with potent activity (IC₅₀ = 18 nM; Kd = 2.9 nM). It inhibits phosphorylation of SMAD2 by selectively targeting ALK4, TGFBR1, and ALK7, key mediators of TGF-β signaling. In vitro, AZ12601011 completely blocks SMAD2 phosphorylation within 20 minutes and suppresses 4T1 mammary tumor cell growth (IC₅₀ = 0.4 μM). In vivo, oral administration (50 mg/kg, twice daily for 25 days) significantly reduces tumor growth and metastasis. With its strong selectivity and efficacy, AZ12601011 is a valuable tool for studying TGF-β signaling and cancer therapeutics.
| CAS Number | 2748337-86-0 |
| Synonyms | 1-(2-pyridin-2-yl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)pyrrolo[3,2-c]pyridine |
| Molecular Formula | C19H15N5 |
| Purity | ≥95% |
| IUPAC Name | 1-(2-pyridin-2-yl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)pyrrolo[3,2-c]pyridine |
| InChI | InChI=1S/C19H15N5/c1-2-9-21-16(5-1)18-22-15-6-3-4-14(15)19(23-18)24-11-8-13-12-20-10-7-17(13)24/h1-2,5,7-12H,3-4,6H2 |
| InChIKey | KQCNNLRNSIXEJU-UHFFFAOYSA-N |
| SMILES | C1CC2=C(C1)N=C(N=C2N3C=CC4=C3C=CN=C4)C5=CC=CC=N5 |
| Chemistry Calculators | Dilution Calculator In vivo Formulation Calculator Molarity Calculator Molecular Weight Calculator Reconstitution Calculator |
