SHP2-D26
Based on 1 publication(s) in Google Scholar
SHP2-D26 is a first, potent and effective SHP2 PROTAC degrader. SHP2-D26 induces SHP2 degradation requires binding to VHL-1 and SHP2 proteins. SHP2-D26 is also neddylation- and proteasome-dependent. SHP2-D26 can be used for the study of esophageal cancer and acute myeloid leukemia.
(Pink: SHP2 ligand (HY-176797); Blue: VHL ligand (HY-150803); Black: linker).
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: 95.83%
- CAS 番号: 2458219-65-1
- 分子式: C56H79ClN12O6S2
- 分子量:1115.89
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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
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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
MedChemExpress（MCE）の使用を引用している文献 SHP2-D26
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生物活性
SHP2[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| KYSE-520 cell line | IC50 |
0.66 μM
Compound: 26; SHP2-D26
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Growth inhibition of human KYSE520 cells measured after 4 days by WST8 assay
Growth inhibition of human KYSE520 cells measured after 4 days by WST8 assay
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[PMID: 32437146] |
| MV4-11 | DC50 |
2.6 nM
Compound: 26; SHP2-D26
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Protac activity at VHL1/SHP2 in human MV4-11 cells assessed as induction of SHP2 degradation measured after 12 hrs by Western blot analysis
Protac activity at VHL1/SHP2 in human MV4-11 cells assessed as induction of SHP2 degradation measured after 12 hrs by Western blot analysis
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[PMID: 32437146] |
| MV4-11 | IC50 |
9.9 nM
Compound: 26; SHP2-D26
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Growth inhibition of human MV4-11 cells measured after 4 days by WST8 assay
Growth inhibition of human MV4-11 cells measured after 4 days by WST8 assay
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[PMID: 32437146] |
SHP2-D26 (0, 3, 10, 30, 100, 300 nM; 12 hours) effectively reduces SHP2 protein in a dosedependent manner, with DC50 values of 6.0 nM, 2.6 nM in KYSE520 and MV-4-11 cells, respectively[1].
SHP2-D26 (100 nM; 0, 2, 4, 8, 12, 24 hours) reduces the SHP2 protein level within 4 h and completes SHP2 depletion with 8 h in KYSE520 and MV-4-11 cells[1].
SHP2-D26 (0-100 μM for KYSE520 cells; 0-10 nM for MV-4-11 cells; 4 days) achieves IC50 values of 0.66 μM, 0.99 nM in KYSE520 and MV-4-11 cells, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:KYSE520 and MV-4-11 cells
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Concentration:0-100 μM for KYSE520 cells; 0-10 nM for MV-4-11 cells
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Incubation Time:4 days
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Result:Achieved IC50 values of 0.66 μM, 0.99 nM in KYSE520 and MV-4-11 cells, respectively.
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Cell Line:KYSE520 and MV-4-11 cells
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Concentration:0, 3, 10, 30, 100, 300 nM
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Incubation Time:12 hours
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Result:Reduced SHP2 protein in a dosedependent manner, with DC50 values of 6.0 and 2.6 nM in KYSE520 and MV-4-11 cells, respectively.
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Cell Line:KYSE520 and MV-4-11 cells
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Concentration:100 nM
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Incubation Time:0, 2, 4, 8, 12, 24 hours
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Result:Reduced the SHP2 protein level within 4 h and completed SHP2 depletion with 8 h.
化学情報
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CAS 番号 2458219-65-1
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性状 Solid
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分子量 1115.89
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分子式 C56H79ClN12O6S2
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Color Off-white to light yellow
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SMILES
ClC(C(SC1=NC=C(N2CCC(N)(CC2)C)N=C1N)=CC=C3)=C3NC(CCC(N(CC4)CCN4CCCCCCCCC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@H](C5)O)C(N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C)=O)=O)=O)=O)=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 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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J Biol Chem
2024 Jul 30:107616. PMID: 39089586
溶剤 & 溶解度
DMSO : 83.33 mg/mL (74.68 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.
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 (272 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
[1]. Wang M, et al. Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein [published correction appears in J Med Chem. 2021 Jan 14;64(1):906-908]. J Med Chem. 2020;63(14):7510-7528. [Content Brief]
[2]. Wang M, et al. Correction to "Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein". J Med Chem. 2021 Jan 14;64(1):906-908. [Content Brief]
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 | 0.8961 mL | 4.4807 mL | 8.9615 mL | 22.4036 mL |
| 5 mM | 0.1792 mL | 0.8961 mL | 1.7923 mL | 4.4807 mL | |
| 10 mM | 0.0896 mL | 0.4481 mL | 0.8961 mL | 2.2404 mL | |
| 15 mM | 0.0597 mL | 0.2987 mL | 0.5974 mL | 1.4936 mL | |
| 20 mM | 0.0448 mL | 0.2240 mL | 0.4481 mL | 1.1202 mL | |
| 25 mM | 0.0358 mL | 0.1792 mL | 0.3585 mL | 0.8961 mL | |
| 30 mM | 0.0299 mL | 0.1494 mL | 0.2987 mL | 0.7468 mL | |
| 40 mM | 0.0224 mL | 0.1120 mL | 0.2240 mL | 0.5601 mL | |
| 50 mM | 0.0179 mL | 0.0896 mL | 0.1792 mL | 0.4481 mL | |
| 60 mM | 0.0149 mL | 0.0747 mL | 0.1494 mL | 0.3734 mL |
SHP2-D26 関連分類
HY-145162 関連分類
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