For research use only. Not for therapeutic Use.
AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC50 of 18 nM and a Kd of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, TGFBR1, and ALK7. AZ12601011 inhibits mammary tumor growth [1].
AZ12601011 (0.01-10 μM; for 20 minutes) completely inhibits Phosphorylation of SMAD2 [1].
AZ12601011 (0.01 µM-10 µM) inhibits the activity of ALK4, ALK7 and TGFBR1 [1].
AZ12601011 inhibits 4T1 cells growth in vitro (IC50=0.4µM) [1].
AZ12601011 (50mg/kg; oral gavage; twice daily; for 25 days) inhibits tumour growth and metastasis in vivo[1].
| Catalog Number | I045994 |
| 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% |
| 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 |
| Reference | [1]. Spender LC, et al. Preclinical Evaluation of AZ12601011 and AZ12799734, Inhibitors of Transforming Growth Factor βSuperfamily Type 1 Receptors. Mol Pharmacol. 2019 Feb;95(2):222-234. |
