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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. Find out more about compound libraries available from Tocris.
M. Wt | 500.35 |
Formula | C24H20Cl2FN5O2 |
Storage | Store at -20°C |
Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 50.03 | 100 | |
ethanol | 12.51 | 25 |
The following data is based on the product molecular weight 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.
Concentration / Solvent Volume / Mass | 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 |
References are publications that support the biological activity of the product.
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.
Keywords: 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
Citations are publications that use Tocris products. Selected citations for TCS ERK 11e include:
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
Do you know of a great paper that uses TCS ERK 11e from Tocris? Please let us know.
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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!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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.