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OrganRegen A-83-01（C909910）

產(chǎn)品中心 > 類器官小分子 > OrganRegen A-83-01（C909910）

OrganRegen A-83-01（C909910）

A-83-01
貨號：C909910
規(guī)格：50mg
品牌：OrganRegen
價格： ￥3940.00
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50mg

A-83-01

貨號：C909910

規(guī)格：50mg

品牌：OrganRegen


產(chǎn)品介紹

DESCRIPTION

Background


A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively[1].


M. W t

421.52


Formula

C97H124N20O31S


CAS No

10047-33-3


Storage

Powder

-20°C  3 years


Solubility

DMSO

41.67 mg/mL(98.86 mM; Need ultrasonic)


H2O

< 0.1 mg/mL(insoluble)                            


 

 

技術(shù)參數(shù)

BIOLOGICAL ALTIVITY

In Vitro   

A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, reduces the level of ALK-5-induced transcription with an IC50 of 12 nM in Mv1Lu cells, also blocks the ALK4-TD and ALK7-TD induced transcription with IC50s of 45 nM and 7.5 nM in R4-2 cells, and weakly suppresses that induced by constitutively active ALK-6, ALK-2, ALK-3, and ALK-1. A 83-01 (0.03-10 μM) potently prevents the growth-inhibitory effects of TGF-β, and completely inhibits the effect at 3 μM. A 83-01 (1-10 μM) inhibits TGF-β-induced Smad activation in HaCaT cells[1]. A 83-01 (1 μM) decreases cell motility, adhesion and invasion increased by TGF-β1 in HM-1 cells, but does not change cell proliferation[2].

In Vivo  

A 83-01 (50, 150 and 500 μg/mouse, i.p.) significantly improves survival of the mice without body weight or neurobehavioral appearances[2]. A 83-01 (0.5 mg/kg, i.p.) shows a significantly strong antitumor effect in mice bearing M109 cells[3].

REFERENCES

[1]. Tojo M, et al. The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-beta. Cancer Sci. 2005 Nov;96(11):791-800.

[2]. Yamamura S, et al. The activated transforming growth factor-beta signaling pathway in peritoneal metastases is a potential therapeutic target in ovarian cancer. Int J Cancer. 2012 Jan 1;130(1):20-8.

[3]. Taniguchi Y, et al. Enhanced antitumor efficacy of folate-linked liposomal Adriamycin with TGF-β type I receptor inhibitor. Cancer Sci. 2010 Oct;101(10):2207-13.