AMPTX-1
Based on 1 Customer Validation
AMPTX-1 is a selective, orally active, covalent reversible BRD9 molecular glue degrader with a DC50 of 0.05 nM. AMPTX-1 selectively recruits BRD9 to the E3 ligase DCAF16. AMPTX-1 forms a ternary complex with BRD9 and a reversible covalent adduct with Cys58 on the surface of DCAF16. AMPTX-1 mediates BRD9 degradation via the proteasome and Cullin RING E3 ligase pathways. AMPTX-1 can be used in the research of solid tumors and hematological malignancies.
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: 98.00%
- CAS 番号: 3033019-04-1
- 分子式: C42H53N5O4
- 分子量:691.90
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保管条件:Powder -20°C, 3 years , 4°C, 2 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
生物活性
AMPTX-1 (6 h) potently degrades endogenous BRD9 in MV4-11 cells (DC50 = 0.5 nM, Dmax = 93%) and MCF-7 cells (DC50 = 2 nM, Dmax = 70%) following 6 h treatment, with a hook effect at concentrations above 100 nM[1].
AMPTX-1 (6 h) -induced BRD9 degradation in BRD9-HiBiT HEK293 cells is dependent on proteasome function, Cullin RING E3 ligase activity, and BRD9 engagement, as pre-treatment with MLN4924, Bortezomib, or BI-7273 blocks degradation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 3033019-04-1
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性状 Solid
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分子量 691.90
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分子式 C42H53N5O4
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Color White to off-white
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SMILES
N#C/C(C(N1CCC2=C(C1C)C=CC=C2CN3CCN(CC34CC4)CC5=C(OC)C=C(C6=CN(C)C(C(C)=C6C)=O)C=C5OC)=O)=C\C(C)(C)C
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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 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : ≥ 100 mg/mL (144.53 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (271 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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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 | 1.4453 mL | 7.2265 mL | 14.4530 mL | 36.1324 mL |
| 5 mM | 0.2891 mL | 1.4453 mL | 2.8906 mL | 7.2265 mL | |
| 10 mM | 0.1445 mL | 0.7226 mL | 1.4453 mL | 3.6132 mL | |
| 15 mM | 0.0964 mL | 0.4818 mL | 0.9635 mL | 2.4088 mL | |
| 20 mM | 0.0723 mL | 0.3613 mL | 0.7226 mL | 1.8066 mL | |
| 25 mM | 0.0578 mL | 0.2891 mL | 0.5781 mL | 1.4453 mL | |
| 30 mM | 0.0482 mL | 0.2409 mL | 0.4818 mL | 1.2044 mL | |
| 40 mM | 0.0361 mL | 0.1807 mL | 0.3613 mL | 0.9033 mL | |
| 50 mM | 0.0289 mL | 0.1445 mL | 0.2891 mL | 0.7226 mL | |
| 60 mM | 0.0241 mL | 0.1204 mL | 0.2409 mL | 0.6022 mL | |
| 80 mM | 0.0181 mL | 0.0903 mL | 0.1807 mL | 0.4517 mL | |
| 100 mM | 0.0145 mL | 0.0723 mL | 0.1445 mL | 0.3613 mL |
AMPTX-1 関連分類
HY-172615 関連分類
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