AZ 12799734

Pricing Availability   Qty
说明: Potent TGF-βRI inhibitor
化学名: 4-[[4-[(2.6-Dimethyl-3-pyridinyl)oxy]-2-pyridinyl]amino]benzenesulfonamide
纯度: ≥98% (HPLC)
说明书
引用文献
评论
文献 (3)
通路 (1)

生物活性 for AZ 12799734

AZ 12799734 is a potent inhibitor of transforming growth factor-β type I receptor (TGF-βRI; ALK5) (IC50 = 17 nM in cellular inhibition assay and 47 nM in TGF-β-induced luciferase activity assay). Also inhibits ALK4, ALK6 and ALK7 at concentrations under 10 μM. Inhibits BMP signaling, phosphorylation of SMAD1 and SMAD2, and TGF-β-induced epithelial cell migration in vitro. Displays cardiotoxicity in vivo. Orally bioavailable.

化合物库 for AZ 12799734

AZ 12799734 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。

技术数据 for AZ 12799734

分子量 370.43
公式 C18H18N4O3S
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 1117684-36-2
PubChem ID 25192277
InChI Key UEOZXMAOIHDDQE-UHFFFAOYSA-N
Smiles CC1=NC(C)=C(OC2=CC=NC(NC3=CC=C(C=C3)[S](N)(=O)=O)=C2)C=C1

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for AZ 12799734

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 37.04 100

制备储备液 for AZ 12799734

以下数据基于产品分子量 370.43。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 2.7 mL 13.5 mL 27 mL
5 mM 0.54 mL 2.7 mL 5.4 mL
10 mM 0.27 mL 1.35 mL 2.7 mL
50 mM 0.05 mL 0.27 mL 0.54 mL

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参考文献 for AZ 12799734

参考文献是支持产品生物活性的出版物。

Goldberg et al (2009) Rapid generation of a high quality lead for transforming growth factor-beta (TGF-beta) type I receptor (ALK5). J.Med.Chem. 52 7901 PMID: 19736928

Anderton et al (2011) Induction of heart valve lesions by small-molecule ALK5 inhibitors. Toxicol.Pathol. 39 916 PMID: 21859884

Spender et al (2019) Preclinical evaluation of AZ12601011 and AZ12799734, inhibitors of transforming growth factor β superfamily type 1 receptors. Mol.Pharmacol. 95 222 PMID: 30459156


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关键词: AZ 12799734, AZ 12799734 supplier, AZ12799734, TGF-beta, RI, TGF-betaRI, ALK5, transforming, growth, factor, beta, receptor, type, 1, cell, migration, Receptors, 6870, Tocris Bioscience

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该领域的文献

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Pathways for AZ 12799734

TGF-β Signaling Pathway

TGF-β Signaling Pathway

The TGF-β signaling pathway is involved in the regulation of growth and proliferation of cells along with migration, differentiation and apoptosis.