PVD-06
Based on 1 Customer Validation
PVD-06 is a selective PROTAC PTPN2 degrader with a DC50 of 217 nM (selectivity index >60-fold over PTP1B). PVD-06 induces PTPN2 degradation via a VHL-, ubiquitin, and proteasome-dependent pathway. PVD-06 can promote T cell activation and amplify IFN-γ-mediated anticancer activity. PVD-06 can be used to further investigate PTPN2 in diseases such as leukemia and melanoma.
(Pink: PTPN2 ligand (HY-168691); Blue: VHL ligand (HY-112078); Black: linker (HY-B0236)).
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- Pureté: 98.30%
- CAS No.: 3032975-48-4
- Formule: C48H55F4N9O11S2
- Masse moléculaire:1074.13
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
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Activité biologique
PTPN2[1]
PVD-06 (0.1-10 μM, 1-48 h) induces PTPN2 degradation and reduces the PTPN2 protein levels through a VHL-, ubiquitin, and proteasome-dependent pathway[1].
PVD-06 (0.1-10 μM, 1-48 h) enhances the phosphorylation of STAT1 in Jurkat cells, a key downstream signaling node, confirming that the effect is dependent on selective PTPN2 degradation[1].
PVD-06 (1.25-5 μM, 3 days) promotes T cell proliferation under CD3/CD28 stimulation in a concentration-dependent manner[1].
PVD-06 (1.25-5 μM, 96 h) significantly amplifies B16F10 cell growth inhibition in a concentration-dependent manner in the presence of IFN-γ[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Jurkat, B16F10, HepG2 and mouse spleen cells
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Concentration:0.1, 0.013, 0.04, 0.12, 0.37, 1, 1.1, 3.5, 5, 10 and 50 μM
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Incubation Time:24 h
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Result:Induced PTPN2 degradation in a concentration-dependent manner without the hook effect.
Showed excellent PTPN2 subtype selectivity in B16F10 and mouse spleen cell models, consistent with the experimental results in the Jurkat cells.
Induced remarkable PTPN2 degradation without affecting the levels of PTP1B, SHP-1, and SHP-2.
Induced PTPN2 degradation on the HepG2 cell line, but it did not affect the PTP1B level.
Significantly reduced the PTPN2 level but not the PTP1B level in mouse spleen cells.
Significantly induced PTPN2 degradation in B16F10 cells, while the PTP1B level remained unchanged.
Dose dependently increased STAT1 phosphorylation after 24 h on the Jurkat cell line in the presence of 10 ng/mL IFN-γ.
Increased STAT1 phosphorylation by degrading PTPN2 selectively.
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Cell Line:Jurkat cells
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Concentration:1 μM
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Incubation Time:1, 2, 3, 6, 9, 12, 24, 36, and 48 h
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Result:Induced PTPN2 degradation in a time-dependent manner without affecting the PTP1B level at all time points.
The degradation induced was weakened by the addition of excessive PTPN2 ligand M8, proteasome inhibitor MG132 (HY-13259), NEDD8-activating enzyme inhibitor MLN4924 (HY-70062), or VHL E3 ligase ligand VM5.
Induced degradation through the PTPN2 ligand-dependent and VHL-dependent ubiquitin proteasomal degradation pathway.
Chemical Information
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CAS No. 3032975-48-4
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Appearance Solid
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Masse moléculaire 1074.13
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Formule C48H55F4N9O11S2
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Color White to off-white
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SMILES
OC(C(F)(F)F)=O.O=C(CN1N=CC(C2=CC=C3C=C(C(N4CC(NS4(=O)=O)=O)=C(C3=C2)F)O)=C1)NCCCCCC(N[C@@H](C(C)(C)C)C(N5C[C@H](O)C[C@H]5C(N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C)=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
Solvant et solubilité
DMSO : 100 mg/mL (93.10 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.33 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.33 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (278 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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Instruction de manipulation (2659 KB)
Références
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 |
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| DMSO | 1 mM | 0.9310 mL | 4.6549 mL | 9.3099 mL | 23.2747 mL |
| 5 mM | 0.1862 mL | 0.9310 mL | 1.8620 mL | 4.6549 mL | |
| 10 mM | 0.0931 mL | 0.4655 mL | 0.9310 mL | 2.3275 mL | |
| 15 mM | 0.0621 mL | 0.3103 mL | 0.6207 mL | 1.5516 mL | |
| 20 mM | 0.0465 mL | 0.2327 mL | 0.4655 mL | 1.1637 mL | |
| 25 mM | 0.0372 mL | 0.1862 mL | 0.3724 mL | 0.9310 mL | |
| 30 mM | 0.0310 mL | 0.1552 mL | 0.3103 mL | 0.7758 mL | |
| 40 mM | 0.0233 mL | 0.1164 mL | 0.2327 mL | 0.5819 mL | |
| 50 mM | 0.0186 mL | 0.0931 mL | 0.1862 mL | 0.4655 mL | |
| 60 mM | 0.0155 mL | 0.0776 mL | 0.1552 mL | 0.3879 mL | |
| 80 mM | 0.0116 mL | 0.0582 mL | 0.1164 mL | 0.2909 mL |
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