AZ12601011 |
| Catalog No.GC60610 |
AZ12601011은 IC50이 18nM이고 Kd가 2.9nM인 경구 활성 선택적 TGFBR1 키나제 억제제입니다. AZ12601011은 ALK4, TGFBR1 및 ALK7을 선택적으로 억제하여 SMAD2의 인산화를 억제합니다. AZ12601011은 유방 종양 성장을 억제합니다.
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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