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Chemical Structure : SIAIS039
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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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.
| M.Wt | 878.41 | |
| Formula | C46H53ClN9O5P | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Jiawen Yang, et al. Bioorg Chem. 2024 Jun 24:150:107590.
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