CW-3308
Based on 1 Customer Validation
CW-3308 is an orally active BRD9 PROTAC degrader with an DC50 of 92 nM. CW-3308 forms a ternary complex with BRD9 and cereblon to mediate BRD9 degradation. CW-3308 inhibits the viability of synovial sarcoma and rhabdoid tumor cells. CW-3308 reduces BRD9 protein levels in xenograft tumor tissues and suppresses tumor growth in xenograft models. CW-3308 can be used for the research of synovial sarcoma and rhabdoid tumors.
(Pink: BRD9 ligand (HY-159596); Blue: Cereblon ligand (HY-159597); Black: linker (HY-159598)).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.43%
- CAS. Nr.: 3055592-99-6
- Formel: C45H48N6O8
- Molecular Weight:800.90
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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BRD9 5 nM (IC50) |
Cereblon |
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Cell Line
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Type | Value | Description | References |
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| G-401 | IC50 |
185 nM
Compound: 27; CW-3308
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Inhibition of cell viability in human G-401 cells incubated for 4 days by CellTiter-Glo luminescent cell viability assay
Inhibition of cell viability in human G-401 cells incubated for 4 days by CellTiter-Glo luminescent cell viability assay
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[PMID: 39132814] |
CW-3308 (Compound 27) potently degrades BRD9 in genetically engineered HEK293 CRISPR knock-in cells after 6 h, with a DC50 of 92 nM and a maximum degradation rate of 99%[1].
CW-3308 (0.1-1000 nM; 3 h) potently and selectively degrades BRD9 in G401 and HS-SY-II cells[1].
CW-3308 potently binds to purified BRD9 protein, with an IC50 of 5.0 nM[1].
CW-3308 (185 nM; 4 days) potently inhibits the viability of G401 and HS-SY-II cells, with IC50 values of 185 nM and 2.7 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:G401 rhabdoid tumor cells
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Concentration:0, 0.1, 1, 10, 100, 1000 nM
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Incubation Time:3 h
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Result:Reduced BRD9 protein levels by 30% at 0.1 nM, 68% at 1 nM, 90% at 10 nM, 93% at 100 nM, and 86% at 1000 nM.
No significant degradation of BRD7 or BRD4 was observed at any tested concentration.
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Cell Line:HS-SY-II synovial sarcoma cells
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Concentration:0, 0.1, 1, 10, 100, 1000 nM
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Incubation Time:3 h
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Result:Reduced BRD9 protein levels by 16% at 1 nM, 70% at 10 nM, 98% at 100 nM, and 76% at 1000 nM.
No degradation was observed at 0.1 nM.
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Cell Line:G401 rhabdoid tumor cells
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Concentration:100 nM
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Incubation Time:0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4 h
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Result:Reduced BRD9 protein levels by 77% at 0.5 h, 91% at 1 h, and ≥94% at all time points from 1.5 h to 4 h.
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Cell Line:G401 rhabdoid tumor cells
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Concentration:185 nM
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Incubation Time:4 days
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Result:Inhibited cell growth with an IC50 of 185 nM and a maximum inhibition (Iₘₐₓ) of 90%.
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Cell Line:HS-SY-II synovial sarcoma cells
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Concentration:2.7 μM
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Incubation Time:4 days
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Result:Inhibited cell growth with an IC50 of 2.7 μM and a maximum inhibition (Iₘₐₓ) of 94%.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID mice[1]
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Dosage:50 mg/kg/25, 50 mg/kg
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Administration:p.o.; single dose/daily 5 days/week; 25 days
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Result:Reduced BRD9 protein levels in tumor tissue by 92.5% relative to controls at 3 hours post-dose.
Reduced BRD9 protein levels in tumor tissue by 45% relative to controls at 24 hours post-dose.
Detected high drug concentrations in plasma and tumor tissue at 3 hours, with low concentrations present at 24 hours.
Achieved a maximum tumor growth inhibition (TGI) of 57% at 25 mg/kg.
Achieved a maximum tumor growth inhibition (TGI) of 60% at 50 mg/kg.
Observed no significant animal weight loss or other signs of toxicity during the study.
Chemical Information
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CAS. Nr. 3055592-99-6
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Appearance Solid
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Molecular Weight 800.90
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Formel C45H48N6O8
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Color White to light yellow
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SMILES
O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=C4C(CN(CC(CC5)CCC65CCN(C(C7=C(OC)C=C(C(C8=CC=NC=C98)=CN(CC)C9=O)C=C7OC)=O)CC6)C4)=C3)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 4.17 mg/mL (5.21 mM; ultrasonic and warming and heat to 60°C; 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
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 | 1.2486 mL | 6.2430 mL | 12.4860 mL | 31.2149 mL |
| 5 mM | 0.2497 mL | 1.2486 mL | 2.4972 mL | 6.2430 mL |
CW-3308 Related Classifications
HY-159579 Related Classifications
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