AZ12601011 B

Research use only, not for human use.

AZ12601011 is an orally active, selective and potent TGFBR1 kinase inhibitor.

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 .

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) . Western Blot Analysis Cell Line:NIH3T3, HaCaT, C2C12, T47D cells Concentration:0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM Incubation Time:20 minutes Result:Completely inhibited Phosphorylation of SMAD2.

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.

——

Angiogenesis

ALK

ALK | TGF-beta/Smad

——

——

2748337-86-0

313.36

C19H15N5

>98% (HPLC)

In Vitro:?DMSO : 5 mg/mL (15.96 mM; Ultrasonic )

N=1C=CC2=C(C1)C=CN2C3=NC(=NC4=C3CCC4)C5=NC=CC=C5

——

(-20℃)

With Ice Pack

≥ 2 years