SIA​​IS039

Overview

SIAIS039 is an orally active c-ros oncogene 1 (ROS1) -specific PROTAC with DC 50 s of 154.46 nM, 126.47 nM, 143.69 nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis , and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib ( HY-12857 ), a linker EM-12 ( HY-138793 ), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib ; Blue: VHL ligand; Black: linker).

Application

Products | Products > Disease Areas > Cancer | Products > Signaling Pathways > PROTAC | Products > Signaling Pathways > Protein Tyrosine Kinase/RTK | Products > Signaling Pathways > Apoptosis | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Research Areas > Cancer > Cancer Metabolism and Metastasis | Products > Research Areas > Cancer | Products > Signaling Pathways > PROTACs | Products > Signaling Pathways > ROS Kinase | Products > Signaling Pathways > Apoptosis

Product Information

• Catalog No.: HY-159147
• CAS No.: 2570251-69-1
• Molecular Formula: C46H53ClN9O5P
• Molecular Weight: 878.40
• Purity: 99.68%
• Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
• Availability: In-stock

Source

Original product source