Product Description: SIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific PROTAC with DC50s 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 E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker)[1].
Applications: Cancer-Kinase/protease
Formula: C46H53ClN9O5P
References: [1]Jiawen Yang, et al. Discovery of a first-in-class protein degrader for the c-ros oncogene 1 (ROS1). Bioorg Chem. 2024 Sep:150:107590.
CAS Number: 2570251-69-1
Molecular Weight: 878.40
Research Area: Cancer
Target: Apoptosis;PROTACs;ROS Kinase
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