SIAIS039 [CAS 2570251-69-1]

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 , a linker EM-12 (HY-138793), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker).

[2570251-69-1]

C46H53ClN9O5P

878.4

O=C(C(N(CC1=C2C=CC=C1C#CCCCN3CCN(C4CCN(C5=CC=C(NC6=NC=C(Cl)C(NC7=CC=CC=C7P(C)(C)=O)=N6)C(OC)=C5)CC4)CC3)C2=O)CC8)NC8=O

Apoptosis; PROTACs; ROS Kinase

Cereblon

99.68

DMSO : 100 mg/mL (ultrasonic)

-20°C, 3 years; 4°C, 2 years (Powder)

Room Temperature