MK-8353

• CAT Number: I020106
• CAS Number: 1184173-73-6
• Molecular Formula: C₃₇H₄₁N₉O₃S
• Molecular Weight: 691.84
• Purity: ≥95%
• Target: Stem Cell/Wnt
• Storage: 2-8°C
• IUPAC Name: (3S)-3-methylsulfanyl-1-[2-[4-[4-(1-methyl-1,2,4-triazol-3-yl)phenyl]-3,6-dihydro-2H-pyridin-1-yl]-2-oxoethyl]-N-[3-(6-propan-2-yloxypyridin-3-yl)-1H-indazol-5-yl]pyrrolidine-3-carboxamide
• InChI: InChI=1S/C37H41N9O3S/c1-24(2)49-32-12-9-28(20-38-32)34-30-19-29(10-11-31(30)41-42-34)40-36(48)37(50-4)15-18-45(22-37)21-33(47)46-16-13-26(14-17-46)25-5-7-27(8-6-25)35-39-23-44(3)43-35/h5-13,19-20,23-24H,14-18,21-22H2,1-4H3,(H,40,48)(H,41,42)/t37-/m0/s1
• InChIKey: KPQQGHGDBBJGFA-QNGWXLTQSA-N
• SMILES: CC(C)OC1=NC=C(C=C1)C2=NNC3=C2C=C(C=C3)NC(=O)C4(CCN(C4)CC(=O)N5CCC(=CC5)C6=CC=C(C=C6)C7=NN(C=N7)C)SC

MK-8353（Cat No.:I020106）, also known as SCH900353, is a selective and orally bioavailable inhibitor of extracellular signal-regulated kinases (ERKs). In vitro studies have shown that MK-8353 effectively inhibits activated ERK1 and ERK2 with IC50 values of 23nM and 8.8nM, respectively, as determined by IMAP kinase assay. Additionally, in a MEK1-ERK2 coupling assay, MK-8353 demonstrates potent inhibition of inactive ERK2 with an IC50 value of 0.5nM. These findings highlight the potential of MK-8353 as a targeted therapeutic agent for diseases driven by dysregulated ERK signaling, including certain types of cancers and other proliferative disorders.

Reference

[1]. Moschos SJ, et al. Development of MK-8353, an orally administered ERK1/2 inhibitor, in patients with advanced solid tumors. JCI Insight. 2018 Feb 22;3(4). pii: 92352.