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
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M.Wt
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878.41
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Formula
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C46H53ClN9O5P
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Jiawen Yang, et al. Bioorg Chem. 2024 Jun 24:150:107590.
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