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)).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.43%
- CAS 番号: 3055592-99-6
- 分子式: C45H48N6O8
- 分子量:800.90
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保管条件: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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Epigenetics Compound Library
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Histone Modification Research Compound Library
HY-L024
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Anti-Cancer Compound Library
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Orally Active Compound Library
HY-L061
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Anti-Blood Cancer Compound Library
HY-L079
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PROTAC Library
HY-L151
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Anti-Hematopathy Compound Library
HY-L171
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Multi-Target Compound Library
HY-L176
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
PROTACs アイソフォーム固有の製品をすべて表示
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生物活性
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BRD9 5 nM (IC50) |
Cereblon |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 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.
化学情報
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CAS 番号 3055592-99-6
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性状 Solid
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分子量 800.90
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (276 KB)
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SDS (252 KB)
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取扱説明書 (2659 KB)
参考文献
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 関連分類
HY-159579 関連分類
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