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编 号:F741753
分子式:C19H15N5
分子量:313.36
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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生物活性:
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 .

体内研究:
AZ12601011 (50mg/kg; oral gavage; twice daily; for 25 days) inhibits tumour growth and metastasis in vivo. Animal Model:Female BALB/c mice at greater than 18g with tumour
Dosage:50mg/kg
Administration:Oral gavage; twice daily; for 25 days
Result:Inhibited tumour growth and metastasis in vivo.

体外研究:
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 (IC50=0.4μM) .
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