SIAIS039 | ROS1 PROTAC | Probechem Biochemicals

Chemical Structure : SIAIS039

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SIAIS039 (SIAIS 039)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	878.41
分子式	C46H53ClN9O5P
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

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

SIAIS039 (SIAIS 039)

生物&药学活性

物理化学性质&存储条件

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SIAIS039 (SIAIS 039)

生物&药学活性

物理化学性质&存储条件

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