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 ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib, Blue: VHL ligand, Black: linker)[1].
Molecular Weight:
878.40
Purity:
99.68
CAS Number:
[2570251-69-1]
Formula:
C46H53ClN9O5P
Target:
Apoptosis,PROTACs,ROS Kinase
Application Notes:
MCE Product type: Reference compound
* VAT and and shipping costs not included. Errors and price changes excepted
