| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Targets |
Povorcitinib phosphate targets Janus kinase 1 (JAK1). JAK1 is a member of the JAK family of tyrosine kinases that plays a critical role in cytokine signaling and inflammation. By selectively inhibiting JAK1, it modulates the inflammatory response. It shows a ~52-fold selectivity for JAK1 over JAK2.
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| ln Vitro |
In vitro, Povorcitinib phosphate is a potent inhibitor of JAK1 with an IC50 of 8.9 nM. Its selectivity is demonstrated by its much weaker inhibition of JAK2 (IC50 = 463 nM). This activity is typically measured in cell-free kinase assays using recombinant JAK enzymes.
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| ln Vivo |
In vivo, Povorcitinib phosphate has demonstrated efficacy in reducing abscesses and inflammatory nodules. It is being developed as an oral therapeutic for inflammatory skin conditions. Its in vivo efficacy would be evaluated in animal models of skin inflammation.
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| Enzyme Assay |
Non-cellular assays for Povorcitinib phosphate involve measuring its inhibition of JAK1 kinase activity. In a typical assay, recombinant JAK1 enzyme is incubated with a substrate peptide and ATP in the presence of varying concentrations of the compound. The phosphorylation of the substrate is measured, and the IC50 is calculated from the dose-response curve.
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| Cell Assay |
In vitro cellular assays for Povorcitinib phosphate assess its ability to inhibit JAK1-mediated signaling in cells. Cells are stimulated with a cytokine that signals through JAK1 (e.g., IFN-γ or IL-6). The effect of the compound on downstream signaling, such as STAT phosphorylation, is measured by Western blotting or ELISA.
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| Animal Protocol |
In vivo animal studies for Povorcitinib phosphate are not extensively detailed in standard product information. As a preclinical compound, its efficacy would be evaluated in animal models of inflammatory skin disease. Endpoints would include measures of skin inflammation, such as lesion size and histological analysis.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of Povorcitinib phosphate are characteristic of an orally bioavailable small molecule. It is the phosphate salt of the active compound, which is likely used to improve its solubility and bioavailability. Its molecular weight is 605.45.
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| Toxicity/Toxicokinetics |
Specific toxicological data for Povorcitinib phosphate are not provided in standard research product information. As a research-grade compound, its safety profile is not established for general use. It should be handled with standard laboratory precautions.
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| References | |
| Additional Infomation |
Povorcitinib phosphate is a research-grade compound for laboratory use only and is not approved for clinical use. Its CAS number is 1637677-33-8. Its primary application is in immunology and dermatology research to study the JAK-STAT pathway and to evaluate JAK1 inhibition as a therapeutic strategy for inflammatory skin diseases.
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| Molecular Formula |
C23H25F5N7O5P
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|---|---|
| Molecular Weight |
605.45
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| Exact Mass |
605.157
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| CAS # |
1637677-33-8
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| Related CAS # |
1637677-22-5;1637677-33-8 (phosphate);
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| PubChem CID |
86280671
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
41
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| Complexity |
909
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| Defined Atom Stereocenter Count |
1
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| SMILES |
P(O)(O)(O)=O.C(C1(N2N=CC(C3=C(NN=C3C)C)=C2)CN(C2C=C(F)C(C(=O)N[C@@H](C)C(F)(F)F)=CC=2F)C1)C#N
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| InChi Key |
XUQIWHXYCLHHCN-UQKRIMTDSA-N
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| InChi Code |
InChI=1S/C23H22F5N7O.H3O4P/c1-12-20(13(2)33-32-12)15-8-30-35(9-15)22(4-5-29)10-34(11-22)19-7-17(24)16(6-18(19)25)21(36)31-14(3)23(26,27)28;1-5(2,3)4/h6-9,14H,4,10-11H2,1-3H3,(H,31,36)(H,32,33);(H3,1,2,3,4)/t14-;/m0./s1
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| Chemical Name |
4-[3-(cyanomethyl)-3-[4-(3,5-dimethyl-1H-pyrazol-4-yl)pyrazol-1-yl]azetidin-1-yl]-2,5-difluoro-N-[(2S)-1,1,1-trifluoropropan-2-yl]benzamide;phosphoric acid
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| Synonyms |
Povorcitinib phosphate; INCB-54707 phosphate; INCB54707 phosphate; INCB 54707 phosphate; 1637677-33-8; MLO3DS9COC; INCB054,707 PHOSPHATE; INCB-054,707 PHOSPHATE;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~165.17 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.44 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.44 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.44 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6517 mL | 8.2583 mL | 16.5166 mL | |
| 5 mM | 0.3303 mL | 1.6517 mL | 3.3033 mL | |
| 10 mM | 0.1652 mL | 0.8258 mL | 1.6517 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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