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Merck
CN
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主要文件

SML0788

Sigma-Aldrich

A 83-01

≥98% (HPLC), powder, TGF-β RI kinase inhibitor

别名:

3-（6-甲基-2-吡啶基）-N-苯基-4-（4-喹啉基）-1H-吡唑-1-硫代甲酰胺, A-83-01, A83-01

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About This Item

经验公式（希尔记法）:
C25H19N5S
CAS号:
909910-43-6
分子量:
421.52
UNSPSC代码:
12352200
NACRES:
NA.77

产品名称

A 83-01, ≥98% (HPLC)

质量水平

100

方案

≥98% (HPLC)

表单

powder

颜色

white to beige

溶解性

DMSO: 5 mg/mL, clear (warmed)

储存温度

−20°C

SMILES字符串

S=C([n]2nc(c(c2)c4c5c(ncc4)cccc5)c3nc(ccc3)C)Nc1ccccc1

InChI

1S/C25H19N5S/c1-17-8-7-13-23(27-17)24-21(19-14-15-26-22-12-6-5-11-20(19)22)16-30(29-24)25(31)28-18-9-3-2-4-10-18/h2-16H,1H3,(H,28,31)

InChI key

HIJMSZGHKQPPJS-UHFFFAOYSA-N

一般描述

A-83-01 may effectively prevent burn wound contraction without impeding wound closure, due to its ability to inhibit the transforming growth factor-β (TGF-β)-induced rise in myofibroblast population. Additionally, it can hinder TGF-β1-dependent cancer metastasis by suppressing epithelial-mesenchymal transition (EMT) in animals.

应用

A 83-01已被用作转化生长因子β激酶1型受体的抑制剂。
A 83-01 has been used:
  • in the culture medium for organoid formation from dissociated tumor cells,
  • as a component in Dulbecco′s modified Eagle medium/nutrient mixture F-12 (DMEM/F12) for culturing human epidermal stem cells (EpSCs)

生化/生理作用

A 83-01是一种TGFβ激酶/激活素受体样激酶（ALK 5）的抑制剂（IC50= 12nM），可阻止Smad2/3的磷酸化并抑制TGFβ诱导的生长。 A 83-01可阻断Smad2的磷酸化并抑制TGF-β诱导的上皮-间质转化。 此外，A 83-01可抑制由TGFβI型受体ALK-5、活化素IB型受体ALK-4、和结节型I受体ALK-7诱导的转录活性。 A-83-01可诱导新生Nkx2.5-eGFP（+）细胞的扩增。

储存分类代码

11 - Combustible Solids

WGK

WGK 3

从最新的版本中选择一种：

分析证书(COA)

Lot/Batch Number
0000383524
0000383524
0000369551
0000369550
0000257827

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A83-01 inhibits TGF-Β-induced upregulation of Wnt3 and epithelial to mesenchymal transition in HER2-overexpressing breast cancer cells.
Wu Y, et al.
Breast Cancer Research and Treatment, 163(3), 449-460 (2017)
Personalized identification of optimal HIPEC perfusion protocol in patient-derived tumor organoid platform
Forsythe SD, et al.
Annals of Surgical Oncology, 27, 4950-4960 (2020)
Topical application of ALK5 inhibitor A-83-01 reduces burn wound contraction in rats by suppressing myofibroblast population
Sun X, et al.
Bioscience, Biotechnology, and Biochemistry, 78, 1805-1812 (2014)
The Use of Endometrial Cancer Patient?Derived Organoid Culture for Drug Sensitivity Testing Is Feasible
Girda E, et al.
International Journal of Gynecological Cancer : Official Journal of the International Gynecological Cancer Society, 27(8), 1701-1701 (2017)
Eugenia Girda et al.
International journal of gynecological cancer : official journal of the International Gynecological Cancer Society, 27(8), 1701-1707 (2017-07-07)
Patient-derived organoids (PDOs), used in multiple tumor types, have allowed evaluation of tumor characteristics from individual patients. This study aimed to assess the feasibility of applying PDO in vitro culture for endocrine-based and drug sensitivity testing in endometrial cancer. Endometrial
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