AZ12601011是一种具有口服活性的，选择性TGFBR1激酶抑制剂，IC50为18nM，Kd为2.9nM。AZ12601011通过选择性的抑制ALK4，TGFBR1和ALK7来抑制SMAD2的磷酸化。AZ12601011抑制乳腺肿瘤的生长。
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]. Western Blot Analysis[1] Cell Line: NIH3T3, HaCaT, C2C12, T47D cells
AZ12601011 (50mg/kg; oral gavage; twice daily; for 25 days) inhibits tumour growth and metastasis in vivo[1]. Animal Model: Female BALB/c mice at greater than 18g with tumour[1]
[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.
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