VX-11e (TCS ERK 11e) is a potent, selective, and orally bioavailable ERK(Extracellular Signal-Regulated Kinase) inhibitor; antitumor agent.

ERK2:<2 nM(Ki)

在HT29细胞中，VX-11e强效抑制细胞增殖，其IC50为48 nM。[1]

在大鼠和小鼠中，VX-11e展现出良好的口服生物可用性。[1] 在携带人类黑色素瘤RPDX肿瘤的NSG小鼠中，VX-11e（50 mg/kg，口服）能显著抑制pRSK，并抑制肿瘤生长。与BKM120联合使用时，VX-11e能显著增强肿瘤生长抑制效果。[2]

ERK Inhibition Assay: Compounds are assayed for the inhibition of ERK2 by a spectophotometric coupled-enzyme assay. In this assay, a fixed concentration of activated ERK2 (10 nM) is incubated with various concentrations of the compounds in DMSO (2.5%) for 10 min. at 30 °C in 0.1 M HEPES buffer, pH = 7.5, containing 10 mM MgCl2, 2.5 mM phosphoenolpyruvate, 200 μM NADH, 150 μg/mL pyruvate kinase, 50 μg/mL lactate dehydrogenase and 200 μM erktide peptide. The reaction is initiated by the addition of 65 μM ATP. The rate of decrease of absorbance at 340 nM is monitored. The IC50 is evaluated from the data as a function of inhibitor concentr

Cell proliferation is measured by 3H-thymidine incorporation. The cells are plated at a concentration of 10,000 cells/well in a 96-well plate using growth media, RPMI 1640 containing 10% FBS. Serially diluted compounds are added. The cells and compounds are incubated for 48 hours at 37°C incubator. After 48 hours, 0.4 μCi of 3H-thymidine is added to each wells for 8 hours and returned to the 37°C incubator. The cells are harvested using a Tomtec 96-well cell harvester and the CPM is determined using the Wallac 1205 BETAPLATE liquid scintillation counter. The IC50 is the 50% inhibition of contr(Only for Reference)