AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC 50 of 18 nM and a K d of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4 , TGFBR1 , and ALK7 . AZ12601011 inhibits mammary tumor growth.
IC50& Target:ALK4 ALK7
In Vitro:AZ12601011 (0.01-10 μM; for 20 minutes) completely inhibits Phosphorylation of SMAD2. AZ12601011 (0.01 µM-10 µM) inhibits the activity of ALK4, ALK7 and TGFBR1. AZ12601011 inhibits 4T1 cells growth in vitro (IC 50 =0.4µM). MCE has not indep
In Vivo:AZ12601011 (5mg/kg; oral gavage; twice daily; for 25 days) inhibits tumour growth and metastasis in vivo. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female BALB/c mice at greater tha
Biological Activity:AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC 50 of 18 nM and a K d of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4 , TGFBR1 , and ALK7 . AZ12601011 inhibits mammary tumor growth.