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  • A 77-01
A 77-01的可视化放大

A 77-01

A potent ALK5 inhibitor

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A 77-01的二维码
  • 库存: 现货
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  • 10mg
    ¥850.00
    680.00
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  • 25mg
    ¥1562.00
    1250.00
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  • 货号: ajci12096
  • CAS: 607737-87-1
  • 别名: A77-01;A-77-01
  • 分子式: C18H14N4
  • 分子量: 286.33
  • 纯度: >98%
  • 溶解度: ≥ 14.3 mg/mL in DMSO, ≥ 8.84 mg/mL in EtOH with ultrasonic and warming
  • 储存: Store at -20°C
  • 库存: 现货

Background

Transforming growth factor (TGF)-β signaling facilitates tumor growth and metastasis in advanced cancer. Use of inhibitors of TGF-β signaling may thus be a novel strategy for the treatment of patients with such cancer. A-77-01 is a close analogue of A-83-01 and has a very similar biological profile of A-83-01. A-83-01 is found to decompose to A-77-01 under certain circumstances and A-77-01 is likely an active component or metabolite of its prodrug A-83-01.
In vitro: A-77-01 and A-83–01 almost completely inhibited the transcriptional activation induced by the constitutively active TGF-β type I receptor (ALK5-TD). A-77-01 and A-83-01 were five to 10 times more potent than the ALK-5 inhibitor SB-431542. In contrast, treatment with 1 μM A-77-01 or 1 μM A-83-01 had no effects on BMP-induced transcriptional activity. However, A-83-01, but not A-77–01, weakly suppressed the transcriptional activity induced by BMP4 at concentrations above 3 μM. A-83-01 and A-77-01 had weak effects on osmotic shock-induced p38 MAPK activity only at high concentrations. A-83-01 and A-77-01 restored the expression of E-cadherin and repressed that of fibronectin and N-cadherin more efficiently than SB-431542 [1].
In vivo: No animal in-vivo data available currently.
Clinical trial: A-77-01 is currently in the preclinical developlent stage and no clinical data are available.
Reference:
[1] Tojo M, Hamashima Y, Hanyu A, Kajimoto T, Saitoh M, Miyazono K, Node M, Imamura T. The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-beta. Cancer Sci. 2005;96(11):791-800.

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