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Background Information:
Extracellular signal regulated kinase (ERK) is a pivotal enzyme in the pathway downstream of Ras, Raf, and MEK, acting as a central link between multiple signaling pathways. VX-11e (or ERK 11e) is a potent, selective, and orally bioavailable inhibitor of ERK2 with Ki < 2 nM, exhibiting potent cellular activity (IC50=48 nM in an HT29 cell proliferation assay). It is highly selective against a panel of more than 140 other kinases - most notably, GSK3 (Ki = 400nM), AURA (Ki = 540nM), CDK2 (Ki = 850nM), FLT3 (Ki = 1400nM), ROCK1 (Ki = 1400nM), and JNK3 (Ki = 1400nM).
Reference:
1. A.M.Aronov, et al, Structure-Guided Design of Potent and Selective Pyrimidyl pyrrole Inhibitors of Extracellular Signal Regulated Kinase(ERK) Using Conformational Control, J.Med.Chem.2009,52,6362–6368.
APIM050258: VX-11E
CAS No.: 896720-20- 0.
Molecular Formula: C24H20Cl2FN5O2?0.1HCl.
Molecular Weight: 505.
Purity: >99% chem and optical purity (HPLC and Chiral HPLC).
QC: HPLC-MS, 1HNMR, Chiral HPLC, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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