Poseltinib
Based on 2 publication(s) in Google Scholar
Poseltinib (HM71224) is an orally active, selective, irreversible small molecule Bruton tyrosine kinase (BTK) inhibitor. With an IC50 of 1.95 nM. Poseltinib effectively inhibits the signaling mediated by B cell receptors (BCR), Fc receptors (FcR), and Toll-like receptors (TLR). Poseltinib has anti-inflammatory activity and can be used in the research of rheumatoid arthritis.
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- Pureza: 98.11%
- No. CAS: 1353552-97-2
- Fòrmula: C26H26N6O3
- Peso molecular:470.52
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Poseltinib
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Actividad biológica
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TLRs |
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Cell Line
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Type | Value | Description | References |
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| Sf9 | IC50 |
14.6 nM
Compound: HM71224
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Inhibition of recombinant human N-terminal GST-tagged JAK3 (781 to end residues) expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins in presence of ATP by ADP-Glo kinase assay
Inhibition of recombinant human N-terminal GST-tagged JAK3 (781 to end residues) expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins in presence of ATP by ADP-Glo kinase assay
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[PMID: 31866272] |
Poseltinib (0.1-100 nM, 30 min) inhibits BCR and FcR signaling in B cells[1].
Poseltinib (1-1000 nM, 1 h) inhibits the phosphorylation of Btk and its downstream molecules such as PLCγ2, in activated Ramos B lymphoma cells in a dose-dependent manner.
Inhibits the production of tumor necrosis factor (TNF)-α, interleukin (IL)-6, and IL-1β by human monocytes, and osteoclast formation by human monocytes in primary human B cells [2].
BTK, AKT, and PLCγ2 in PBMCs cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:B cells
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Concentration:0.1-100 nM
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Incubation Time:30 min
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Result:Blocked both autophosphorylation of BTK and phosphorylation of PLCγ2 with IC50 values of less than 10 nM. Decreased the production of both TNF-α and IL-6 in a dose-dependent manner.
Poseltinib (1-30 mg/kg p.o, once a day for 2 weeks) improves experimental arthritis in mice [2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MRL/lpr mice and NZB/W F1 mice models[1]
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Dosage:3-30 mg/kg
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Administration:p.o
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Result:Decreased the spleen weights and prevented skin lesion progression. Ameliorated renal injury and inflammation and improved the survival rate.
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Animal Model:Collagen-induced arthritis (CIA) mouse model[2]
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Dosage:1-30 mg/kg
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Administration:p.o
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Result:Reduced the serum IL-6, circulating anti-collagen antibodies and total IgG levels. Reduced erosive bone changes and prevented bone loss.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1353552-97-2
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Appearance Solid
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Peso molecular 470.52
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Fòrmula C26H26N6O3
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Color Light yellow to yellow
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SMILES
O=C(C=C)NC1=CC=CC(OC2=C(OC=C3)C3=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=N2)=C1
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Synonyms
HM71224; LY3337641
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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ACS Pharmacol Transl Sci
Comprehensive Characterization of Bruton's Tyrosine Kinase Inhibitor Specificity, Potency, and Biological Effects: Insights into Covalent and Noncovalent Mechanistic Signatures. [Abstract]2025 Mar 12;8(4):917-931. PMID: 40242575 -
Solvente y solubilidad
DMSO : 100 mg/mL (212.53 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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 7.5 mg/mL (15.94 mM); Clear solution
This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 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.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Kim YY, et al. HM71224, a selective Bruton's tyrosine kinase inhibitor, attenuates the development of murine lupus. Arthritis Res Ther. 2017 Sep 26;19(1):211. [Content Brief]
[2]. Park JK, et al. HM71224, a novel Bruton's tyrosine kinase inhibitor, suppresses B cell and monocyte activation and ameliorates arthritis in a mouse model: a potential drug for rheumatoid arthritis. Arthritis Res Ther. 2016 Apr 18;18:91. [Content Brief]
[3]. Byun JY, et al. Target modulation and pharmacokinetics/pharmacodynamics translation of the BTK inhibitor poseltinib for model-informed phase II dose selection. Sci Rep. 2021 Sep 21;11(1):18671. [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 |
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| DMSO | 1 mM | 2.1253 mL | 10.6265 mL | 21.2531 mL | 53.1327 mL |
| 5 mM | 0.4251 mL | 2.1253 mL | 4.2506 mL | 10.6265 mL | |
| 10 mM | 0.2125 mL | 1.0627 mL | 2.1253 mL | 5.3133 mL | |
| 15 mM | 0.1417 mL | 0.7084 mL | 1.4169 mL | 3.5422 mL | |
| 20 mM | 0.1063 mL | 0.5313 mL | 1.0627 mL | 2.6566 mL | |
| 25 mM | 0.0850 mL | 0.4251 mL | 0.8501 mL | 2.1253 mL | |
| 30 mM | 0.0708 mL | 0.3542 mL | 0.7084 mL | 1.7711 mL | |
| 40 mM | 0.0531 mL | 0.2657 mL | 0.5313 mL | 1.3283 mL | |
| 50 mM | 0.0425 mL | 0.2125 mL | 0.4251 mL | 1.0627 mL | |
| 60 mM | 0.0354 mL | 0.1771 mL | 0.3542 mL | 0.8855 mL | |
| 80 mM | 0.0266 mL | 0.1328 mL | 0.2657 mL | 0.6642 mL | |
| 100 mM | 0.0213 mL | 0.1063 mL | 0.2125 mL | 0.5313 mL |
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