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).
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- Pureté: 95.83%
- CAS No.: 2458219-65-1
- Formule: C56H79ClN12O6S2
- Masse moléculaire:1115.89
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) SHP2-D26
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Activité biologique
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.
Chemical Information
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CAS No. 2458219-65-1
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Appearance Solid
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Masse moléculaire 1115.89
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
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
Solvant et solubilité
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (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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Instruction de manipulation (2659 KB)
Références
[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 Related Classifications
HY-145162 Related Classifications
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