SIAIS039
Based on 1 Customer Validation
SIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific PROTAC with DC50s of 154.46 nM, 126.47 nM, 143.69 nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib (HY-12857), a linker EM-12 (HY-138793), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.68%
- CAS No.: 2570251-69-1
- Formula: C46H53ClN9O5P
- Molecular Weight:878.40
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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Cereblon |
Chemical Information
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CAS No. 2570251-69-1
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Appearance Solid
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Molecular Weight 878.40
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Formula C46H53ClN9O5P
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Color White to off-white
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (113.84 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (268 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.1384 mL | 5.6922 mL | 11.3843 mL | 28.4608 mL |
| 5 mM | 0.2277 mL | 1.1384 mL | 2.2769 mL | 5.6922 mL | |
| 10 mM | 0.1138 mL | 0.5692 mL | 1.1384 mL | 2.8461 mL | |
| 15 mM | 0.0759 mL | 0.3795 mL | 0.7590 mL | 1.8974 mL | |
| 20 mM | 0.0569 mL | 0.2846 mL | 0.5692 mL | 1.4230 mL | |
| 25 mM | 0.0455 mL | 0.2277 mL | 0.4554 mL | 1.1384 mL | |
| 30 mM | 0.0379 mL | 0.1897 mL | 0.3795 mL | 0.9487 mL | |
| 40 mM | 0.0285 mL | 0.1423 mL | 0.2846 mL | 0.7115 mL | |
| 50 mM | 0.0228 mL | 0.1138 mL | 0.2277 mL | 0.5692 mL | |
| 60 mM | 0.0190 mL | 0.0949 mL | 0.1897 mL | 0.4743 mL | |
| 80 mM | 0.0142 mL | 0.0712 mL | 0.1423 mL | 0.3558 mL | |
| 100 mM | 0.0114 mL | 0.0569 mL | 0.1138 mL | 0.2846 mL |
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