2. Protein Tyrosine Kinase/RTK Immunology/Inflammation
  3. Btk BMX Kinase Toll-like Receptor (TLR)
  4. Poseltinib

Poseltinib  (Synonyms: HM71224; LY3337641)

製品番号: HY-109010 純度: 98.11%
COA 取扱説明書 Technical Support

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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Poseltinib

Poseltinib 構造式

CAS 番号 : 1353552-97-2

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 57 在庫あり
Solution
10 mM * 1 mL in DMSO USD 57 在庫あり
Solid
5 mg $55 在庫あり
10 mg $90 在庫あり
25 mg $190 在庫あり
50 mg $350 在庫あり
100 mg $550 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 2 publication(s) in Google Scholar

Other Forms of Poseltinib:

Poseltinib 関連抗体

Top Publications Citing Use of Products

Toll-like Receptor (TLR) アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

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[1][2][3].

IC50 & Target

TLRs

 

Cellular Effect
Cell Line Type Value Description References
Sf9 IC50
14.6 1
Compound: HM71224
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
[PMID: 31866272]
Sf9 IC50
14.6 1
Compound: HM71224
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
[PMID: 31866272]
Sf9 IC50
14.6 1
Compound: HM71224
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
[PMID: 31866272]
体外実験

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.

Poseltinib 関連抗体

Western Blot Analysis[1]

Cell Line: B cells
Concentration: 0.1-100 nM
Incubation Time: 30 min
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.
体内実験

Poseltinib (3,-30 mg/kg, p.o, once a day, from 18 to 40 weeks) reduces the overactivity of B cells by inhibiting BTK, alleviating the development of systemic lupus erythematosus (SLE) and lupus nephritis (LN)[1].
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.

Animal Model: MRL/lpr mice and NZB/W F1 mice models[1]
Dosage: 3-30 mg/kg
Administration: p.o
Result: Decreased the spleen weights and prevented skin lesion progression.
Ameliorated renal injury and inflammation and improved the survival rate.
Animal Model: Collagen-induced arthritis (CIA) mouse model[2]
Dosage: 1-30 mg/kg
Administration: p.o
Result: Reduced the serum IL-6, circulating anti-collagen antibodies and total IgG levels.
Reduced erosive bone changes and prevented bone loss.
臨床実験
分子量

470.52

分子式

C26H26N6O3
CAS 番号
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C=C)NC1=CC=CC(OC2=C(OC=C3)C3=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=N2)=C1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1253 mL 10.6265 mL 21.2531 mL
5 mM 0.4251 mL 2.1253 mL 4.2506 mL
10 mM 0.2125 mL 1.0627 mL 2.1253 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 7.5 mg/mL (15.94 mM); Clear solution

    This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
純度とドキュメンテーション
参考文献

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
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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Poseltinib Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Poseltinib1353552-97-2HM71224 LY3337641HM 71224HM-71224LY3337641LY 3337641LY-3337641BtkBMX KinaseToll-like Receptor (TLR)Bruton tyrosine kinaseExperimental arthritis mouse modelanti-inflammatoryInhibitorinhibitorinhibit

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