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抑制剂描述:

产品名称:A-83-01

产品别名:见爱必信官网

英文别名:A-83-01

靶点:TGF-β Receptor

CAS:909910-43-6

纯度:≥98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

A-83-01 is a selective inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7 with IC50 values of 12 nM, 45 nM and 7.5 nM, respectively.

溶解性:DMSO : 30 mg/mL (71.17 mM; Need ultrasonic)

体外研究:

A-83-01 (4 μM) treatment increases myotube formation, the expression of MyHC and the expression of Myf5 and MyoD in C2C12 cells. Expression of pSmad3 is increased by the addition of TGF-β1, and the effects of TGF-β1 are inhibited in ovarian cancer cells by A-83-01. TGF-β1 increases cell motility, adhesion and invasion, while A-83-01 decreases these behaviors in HM-1 cells. A-83-01 treatment significantly increases these parameters within 24 h that is positively related to pericyte coverage and tumor cell proliferation. Apparent diffusion coefficient (ADC) determined by diffusion-weighed imaging is decreased by A-83-01 treatment, suggesting the decrease of tumor interstitial fluid pressure.

体内研究:A-83-01 (50, 150 and 500 μg/mouse, i.p.) significantly improves survival of the mice without body weight or neurobehavioral appearances. A-83-01 (0.5 mg/kg, i.p.) shows a significantly stronger antitumor effect in mice bearing M109 cells.

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