A 77-01
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
转化生长因子(TGF)-β信号转导促进晚期肿瘤的肿瘤生长和转移。使用TGF-β信号转导抑制剂可能因此成为治疗此类癌症患者的新策略。A-77-01是A-83-01的类似物,且与A-83-01有极其相似的生物学特性。研究发现A-83-01在一定条件下可分解为A-77-01,且A-77-01很可能是其前体药物A-83-01的活性成分或代谢产物。
体外:A-77-01和A-83–01几乎完全抑制由组成性激活突变型TGF-β I型受体(ALK5-TD)诱发的转录激活。A-77-01和A-83-01的抑制效果比ALK-5抑制剂SB-431542的多5到10倍。相反,1 μM的A-77-01或1 μM的A-83-01对BMP诱发的转录激活没有作用。但是,3 μM以上的A-83-01(而非A-77–01)可微弱抑制BMP4诱发的转录激活。高浓度的A-83-01和A-77-01对渗透压休克诱导的p38 MAPK活性的影响很小。A-83-01和A-77-01恢复E-cadherin的表达,且比SB-431542更高效地抑制纤连蛋白和神经钙黏素的表达[1]。
体内:目前还没有动物体内相关数据。
临床试验:目前A-77-01处于临床前发展阶段,还没有临床数据。
参考文献:
[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.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 286.33 |
Cas No. | 607737-87-1 |
Formula | C18H14N4 |
Synonyms | A77-01;A-77-01 |
Solubility | insoluble in H2O; ≥14.3 mg/mL in DMSO; ≥8.84 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | 4-[5-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl]quinoline |
SDF | Download SDF |
Canonical SMILES | CC1=CC=CC(=N1)C2=C(C=NN2)C3=CC=NC4=CC=CC=C34 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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