VX-11E

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.