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Submit ReviewTCS ERK 11e is a potent and selective extracellular signal-related kinase 2 (ERK2) inhibitor (Ki values are <2, 395, 540 and 852 nM for ERK2, GSK-3, Aurora Kinase A and Cdk2 respectively). Potently blocks proliferation of HT29 cells (IC50 = 48 nM). Orally bioavailable.
TCS ERK 11e is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
分子量 | 500.35 |
公式 | C24H20Cl2FN5O2 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 896720-20-0 |
PubChem ID | 11634725 |
InChI Key | WUTVMXLIGHTZJC-OAQYLSRUSA-N |
Smiles | O=C(N[C@H](CO)C3=CC(Cl)=CC=C3)C1=CC(C2=NC(NC4=CC=C(F)C=C4Cl)=NC=C2C)=CN1 |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 50.03 | 100 | |
ethanol | 12.51 | 25 |
以下数据基于产品分子量 500.35。 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.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2 mL | 9.99 mL | 19.99 mL |
5 mM | 0.4 mL | 2 mL | 4 mL |
10 mM | 0.2 mL | 1 mL | 2 mL |
50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
参考文献是支持产品生物活性的出版物。
Aronov et al (2009) Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-related kinase (ERK) using conformational control. J.Med.Chem. 52 6362 PMID: 19827834
If you know of a relevant reference for TCS ERK 11e, please let us know.
关键词: TCS ERK 11e, TCS ERK 11e supplier, TCSERK11e, extracellular, signal, related, kinase, 2, ERK2, inhibitors, inhibits, potent, selective, cell, permeable, orally, bioavailable, VTX11e, VX11e, VX, 11e, ERK, 4465, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 TCS ERK 11e 的部分引用包括:
Rozbeh et al (2014) The cellular thermal shift assay for evaluating drug target interactions in cells. Nat Protoc 9 2100-22 PMID: 25101824
Kai et al (2022) Small Molecule Arranged Thermal Proximity Coaggregation (smarTPCA)-A Novel Approach to Characterize Protein-Protein Interactions in Living Cells by Similar Isothermal Dose-Responses. Int J Mol Sci 23 PMID: 35628420
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.