SIAIS039
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).
Product Specifications
CAS Number
2570251-69-1
UNSPSC
12352005
Target
Apoptosis; PROTACs; ROS Kinase
Type
Reference compound
Related Pathways
Apoptosis; PROTAC; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/sia-is039.html
Purity
99.68
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
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
Molecular Formula
C46H53ClN9O5P
Molecular Weight
878.40
References & Citations
[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
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Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
Cereblon
Available Sizes
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