AZ12601011 |
| カタログ番号GC60610 |
AZ12601011 は、18 nM の IC50 と 2.9 nM の Kd を持つ経口活性の選択的 TGFBR1 キナーゼ阻害剤です。 AZ12601011 は、ALK4、TGFBR1、および ALK7 を選択的に阻害することにより、SMAD2 のリン酸化を阻害します。 AZ12601011 は乳腺腫瘍の増殖を阻害します。
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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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.
Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)
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