Povorcitinib phosphate
Based on 1 Customer Validation
Povorcitinib (INCB54707) phosphate is a potent and selective JAK1 inhibitor that effectively reduces abscesses and inflammatory nodules. Povorcitinib phosphate can be used to study cutaneous lupus erythematosus (CLE) and lichen planus (LP) (information extracted from patent WO2021076124A1).
For research use only. We do not sell to patients.
- Purity: 98.82%
- CAS No.: 1637677-33-8
- Formula: C23H25F5N7O5P
- Molecular Weight:605.45
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Down Syndrome (DS) carrying Dp16 mouse models[4]
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Dosage:60 mg/kg
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Administration:po, twice daily for 16 days
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Result:Improved the survival rate of Dp16 mice.
Reduced the levels of MCP-1, IP-10, IFN-γ, and TNF-α in serum.
Reduced the levels of ALT and AST.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1637677-33-8
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Appearance Solid
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Molecular Weight 605.45
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Formula C23H25F5N7O5P
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Color White to off-white
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SMILES
O=P(O)(O)O.N#CCC1(N2C=C(C3=C(C)NN=C3C)C=N2)CN(C4=C(C=C(C(F)=C4)C(N[C@@H](C)C(F)(F)F)=O)F)C1
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Synonyms
INCB54707 phosphate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL (165.17 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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: ≥ 2.08 mg/mL (3.44 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (3.44 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Purity & Documentation
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Data Sheet (274 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)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[2]. Kirby JS, et al. Efficacy and safety of the oral Janus kinase 1 inhibitor povorcitinib (INCB054707) in patients with hidradenitis suppurativa in a phase 2, randomized, double-blind, dose-ranging, placebo-controlled study. J Am Acad Dermatol. 2023 Oct 21:S0190-9622(23)03037-2. [Content Brief]
[4]. Tuttle KD, et al., JAK1 Inhibition Blocks Lethal Immune Hypersensitivity in a Mouse Model of Down Syndrome. Cell Rep. 2020 Nov 17;33(7):108407. [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 (sealed storage, away from moisture). 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 | 1.6517 mL | 8.2583 mL | 16.5166 mL | 41.2916 mL |
| 5 mM | 0.3303 mL | 1.6517 mL | 3.3033 mL | 8.2583 mL | |
| 10 mM | 0.1652 mL | 0.8258 mL | 1.6517 mL | 4.1292 mL | |
| 15 mM | 0.1101 mL | 0.5506 mL | 1.1011 mL | 2.7528 mL | |
| 20 mM | 0.0826 mL | 0.4129 mL | 0.8258 mL | 2.0646 mL | |
| 25 mM | 0.0661 mL | 0.3303 mL | 0.6607 mL | 1.6517 mL | |
| 30 mM | 0.0551 mL | 0.2753 mL | 0.5506 mL | 1.3764 mL | |
| 40 mM | 0.0413 mL | 0.2065 mL | 0.4129 mL | 1.0323 mL | |
| 50 mM | 0.0330 mL | 0.1652 mL | 0.3303 mL | 0.8258 mL | |
| 60 mM | 0.0275 mL | 0.1376 mL | 0.2753 mL | 0.6882 mL | |
| 80 mM | 0.0206 mL | 0.1032 mL | 0.2065 mL | 0.5161 mL | |
| 100 mM | 0.0165 mL | 0.0826 mL | 0.1652 mL | 0.4129 mL |
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