化合物 T10426 T10426

Product Introduction
Bioactivity


英文名: AZ12601011

描述: AZ12601011 is a highly potent and selective inhibitor of the TGFBR1 kinase, administered orally. It displays an IC50 of 18 nM and a Kd of 2.9 nM. By selectively targeting ALK4, TGFBR1, and ALK7, AZ12601011 effectively inhibits the phosphorylation of SMAD2. Additionally, it has been shown to hinder the growth and metastasis of mammary tumors [1].

体外活性: AZ12601011 (0.01-10 μM; for 20 minutes) entirely 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 (IC 50 =0.4μM) [1]. Western Blot Analysis [1] 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.

体内活性: AZ12601011 (50mg/kg; oral gavage; twice daily; for 25 days) inhibits tumour growth and migration in vivo [1]. Animal Model: Female BALB/c mice at greater than 18g with tumour [1] Dosage: 50mg/kg Administration: Oral gavage; twice daily; for 25 days Result: Inhibited both tumour growth and metastasis in vivo.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 5 mg/mL (15.96 mM)


关键字: AZ12601011 | AZ-12601011 | AZ 12601011

相关产品: Belizatinib | GW788388 | OD36 | A 77-01 | Blu-782 | EML4-ALK kinase inhibitor 1 | Ceritinib dihydrochloride | Ceritinib | Vactosertib Hydrochloride | INCB-000928

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途