APS03118

Overview

APS03118 is an orally active, potent and selective rearranged during transfection ( RET ) inhibitor. APS03118 broadly inhibits RET fusions and mutations (including G810, V804, L730, and Y806 variants), with IC 50 values predominantly below 1 nM (0.095 nM for WT; ranging from 0.00438 to 5.72 nM for mutants), and demonstrates marked superiority against RET G810 mutations. APS03118 inhibits the entire RET signaling pathway (including RET , Shc, and ERK1/2 ), with >20-fold selectivity over most off-target kinases (except FLT3 and YES ). APS03118 induces complete tumor regression in KIF5B-RET and CCDC6-RET V804 M patient derived xenografts (PDXs) and significantly prolongs survival in an intracranial CCDC6-RET metastasis mice model. APS03118 can be used for selective RET inhibitor (SRI)-resistant, RET-driven cancer research.

Application

Products | Products > Disease Areas > Cancer | Products > Disease Areas > Lung Cancer | Products > Signaling Pathways > MAPK/ERK Pathway | Products > Signaling Pathways > Stem Cell/Wnt | Products > Signaling Pathways > Protein Tyrosine Kinase/RTK | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Research Areas > Cancer > Cancer Immunotherapy | Products > Research Areas > Cancer > Cancer Stem Cells | Products > Research Areas > Cancer > Cancer Drug Resistance | Products > Research Areas > Cancer > Cancer Metabolism and Metastasis | Products > Research Areas > Cancer | Products > Signaling Pathways > ERK | Products > Signaling Pathways > RET

Product Information

• Catalog No.: HY-178061
• CAS No.: 2598870-24-5
• Molecular Formula: C27H28N8O2
• Molecular Weight: 496.56
• Purity: 99.98%
• Storage: Please store the product under the recommended conditions in the Certificate of Analysis.
• Availability: In-stock

Source

Original product source