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SIAIS039

Chemical Structure : SIAIS039

CAS No.: 2570251-69-1

SIAIS039 (SIAIS 039)

Catalog No.: PC-22538Not For Human Use, Lab Use Only.

SIAIS039 is the first ROS1-specific PROTAC degrader with DC50 of 154.46 nM in HCC78 cells, shows cytotoxic effects in cells carrying ROS1 fusion mutations.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

SIAIS039 is the first ROS1-specific PROTAC degrader with DC50 of 154.46 nM in HCC78 cells, shows cytotoxic effects in cells carrying ROS1 fusion mutations.
SIAIS039 induced time- and dose-dependent ROS1 degradation with long-lasting effects.
SIAIS039 is a potent and fast-acting ROS1-selective degrader with nanomolar cytotoxic effects on ROS1-positive NSCLC cells.
SIAIS039 inhibited cell proliferation, promoted cell-cycle arrest in G0/G1, induced apoptosis and inhibited colony formation.
SIAIS039 exhibited excellent oral anti-tumor activities with minimal off-target effects in vivo.

Physicochemical Properties

M.Wt 878.41
Formula C46H53ClN9O5P
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-(4-(5-(4-(1-(4-((5-chloro-4-((2-(dimethylphosphoryl)phenyl)amino)pyrimidin-2-yl)amino)-3-methoxyphenyl)piperidin-4-yl)piperazin-1-yl)pent-1-yn-1-yl)-1-oxoisoindolin-2-yl)piperidine-2,6-dione

References

1. Jiawen Yang, et al. Bioorg Chem. 2024 Jun 24:150:107590.

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