DU-14 (PTP1B/TC-PTP PROTAC)
Based on 1 Customer Validation
DU-14 (PTP1B/TC-PTP PROTAC) is a potent and selective PTP1B and TC-PTP dual PROTAC degrader. DU-14 (PTP1B/TC-PTP PROTAC) has the IC50 for PTP1B and TC-PTP phosphatase activity of 24.2 nM and 30.1 nM, respectively. DU-14 (PTP1B/TC-PTP PROTAC) enhances IFN-γ signaling, promotes T cell activation, and has anti-tumor activity.
(Pink: PTP1B ligand (HY-171027); Blue: VHL ligand (HY-112078); Black: linker (HY-W340290)).
For research use only. We do not sell to patients.
- Purity: 99.78%
- CAS No.: 3053413-58-1
- Formula: C74H85BrF2N9O14PS
- Molecular Weight:1505.46
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Storage:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
IC50: 24.2 nM (PTP1B); 30.1 nM (TC-PTP)[1]
DU-14 (PTP1B/TC-PTP PROTAC) (0-1000 nM; 16 h) causes PTP1B/TC-PTP degradation and promotes STAT1 phosphorylation in IFN-γ-treated MC38 cells[1].
DU-14 (PTP1B/TC-PTP PROTAC) (48 h) effectively degrades TC-PTP and PTP1B in T cells and promotes the activation of T cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:IFN-γ treated MC38 cells
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Concentration:0, 5, 25, 125, 250, 500 and 1000 nM
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Incubation Time:16 h
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Result:Inhibited the levels of PTP1B and TC-PTP in a dose-dependent manner.
Increased the level of pSTAT1/Y701 in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice bearing MC38 colorectal tumors in the flanks[1]
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Dosage:25 and 50 mg/kg
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Administration:Intraperitoneal injection (i.p.); 10 days
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Result:Effectively repressed MC38 tumor growth at dose of 25 mg/kg, and resulted in static tumor growth at dose of 50 mg/kg.
Did not produce significant toxicity.
Degraded nearly complete PTP1B and TC-PTP in whole tumor homogenates.
Increased CD8+ T cell infiltrates in MC38 tumors.
Chemical Information
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CAS No. 3053413-58-1
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Appearance Solid
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Molecular Weight 1505.46
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Formula C74H85BrF2N9O14PS
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Color White to off-white
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SMILES
O=P(O)(O)C(F)(F)C(C=C1)=CC=C1C[C@H](NC([C@@H](NC(CC2=CC(OC)=C(C=C2)O)=O)CC3=CC=CC=C3)=O)C(N[C@@H](CCCCNC(C4=CC(Br)=C(C=C4)C)=O)C(NCC5=CC=CC(CC(N[C@@H](C(C)(C)C)C(N6[C@@H](C[C@H](C6)O)C(N[C@H](C7=CC=C(C8=C(N=CS8)C)C=C7)C)=O)=O)=O)=C5)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
DMSO : 100 mg/mL (66.42 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 (protect from light, stored under nitrogen). 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 (protect from light, stored under nitrogen). 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)
Purity & Documentation
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Data Sheet (275 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)
References
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 (protect from light, stored under nitrogen). 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 |
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| DMSO | 1 mM | 0.6642 mL | 3.3212 mL | 6.6425 mL | 16.6062 mL |
| 5 mM | 0.1328 mL | 0.6642 mL | 1.3285 mL | 3.3212 mL | |
| 10 mM | 0.0664 mL | 0.3321 mL | 0.6642 mL | 1.6606 mL | |
| 15 mM | 0.0443 mL | 0.2214 mL | 0.4428 mL | 1.1071 mL | |
| 20 mM | 0.0332 mL | 0.1661 mL | 0.3321 mL | 0.8303 mL | |
| 25 mM | 0.0266 mL | 0.1328 mL | 0.2657 mL | 0.6642 mL | |
| 30 mM | 0.0221 mL | 0.1107 mL | 0.2214 mL | 0.5535 mL | |
| 40 mM | 0.0166 mL | 0.0830 mL | 0.1661 mL | 0.4152 mL | |
| 50 mM | 0.0133 mL | 0.0664 mL | 0.1328 mL | 0.3321 mL | |
| 60 mM | 0.0111 mL | 0.0554 mL | 0.1107 mL | 0.2768 mL |
DU-14 (PTP1B/TC-PTP PROTAC) Related Classifications
HY-164864 Related Classifications
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