Fig. 1 · Structure
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SIAIS039
ROS1 PROTAC
SIAIS039 is an orally active PROTAC targeting the c-ros oncogene 1 (ROS1), exhibiting DC50 values of 154.46 nM, 126.47 nM, and 143.69 nM in HCC78 cells, and Ba/F3 cells expressing the CD74-ROS1 and SDC4-ROS1 fusions, respectively. This compound effectively suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity in ROS1-positive cells. Additionally, SIAIS039 demonstrates significant anti-tumor effects in vivo against ROS1-driven tumor growth, making it a valuable tool for research in targeted cancer therapy.
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Specifications
| Manufacturer | Adooq Bioscience |
|---|---|
| Actions | Degrader |
| CAS Number | 2570251-69-1 |
| Applications | ROS1 PROTAC |
| Formula | C46H53ClN9O5P |
| Molecular Weight | 878.40 |
| 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 |
Storage & Solubility
In Vitro Solubility
Reported Solubility
No reported solubility data are available for this product.
Preparing Stock Solutions
| Concentration | |
|---|---|
Values use four significant digits. Prepare to the final solution volume; this is not the volume of solvent to add.
Stock preparation is unavailable for this product molecular weight.
Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.
Storage
Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.