Art. -Nr.: HY-151808

JS25

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JS25 is a selective and covalent inhibitor of BTK that inactivates BTK with an IC₅₀ value of 5.8 nM by chelating Tyr551. JS25 inhibits cancer cells proliferation, pronounces cell death, and promotes murine xenograft model of Burkitt’s lymphoma. JS25 effectively crosses the blood-brain barrier.

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Reinheit: 98.37%
CAS. Nr.: 2411771-95-2
Formel: C₂₉H₂₄N₄O₄S
Molecular Weight:524.59

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

JS25 Chemical Structure

CAS. Nr.: 2411771-95-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 5.8 nM (BTK), 49.0 nM (BMX), 440 nM (ITK), 190 nM (TXK), 220 nM (TEC), 2.60 μM (BLK)^[1]

In Vitro

JS25 (0-50 μM; 72 h) inhibits the proliferation of myeloid and lymphoid B-cell cancer cell lines^[1].
JS25 shows inhibitory capability against BTK, BMX, ITK, TXK, TEC, and BLK with IC₅₀s of 28.5 nM, 49.0 nM, 0.44 μM, 0.19 μM, 0.22 μM, and 2.60 μM, respectively; shows little inhibition against other BTK pathway-related proteins (EGFR, ERBB2, and JAK3), with IC₅₀>3 μM. JS25 presents a more favorable selectivity profile than Ibrutinib (HY-10997) and Acalabrutinib (HY-17600)^[1].
JS25 (10 μM; 0, 4, 15 h) degrades BTK and inhibits both the catalytic activity and the expression of BTK in tumor cells^[1].
JS25 (10 μM; 72 h) inhibits the tumor growth of Burkitt’s lymphoma and induces selective ex vivo cytotoxicity in primary diffuse large B-cell lymphoma (DLBCL) samples^[1].
JS25 (15 μM) shows 28.5% perme-ability to the BBB at 24 h in HBEC-5i cell model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

JS25 (10 mg/kg and 20 mg/kg; i.p.; every 2 days, for 14 d) inhibits tumor growth and results a significant reduction in their secondary tumor formation in murine xenograft model of Burkitt’s lymphoma^[1].
JS25 (1, 2.5, and 5 μM; injection; every day for 2 days) decreases tumor burden in zebrafish-derived xenografts of chronic lymphocytic leukemia, wich efficacy is better than Ibrutinib (HY-10997)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female adult BALB/c/NSG mice with Raji cells (s.c.)^[1]
Dosage:

10 mg/kg and 20 mg/kg
Administration:

Intraperitoneal injection; every 2 days for 14 days
Result:

Caused a 30-40% reduction of the subcutaneous tumor and an overall reduction in the percentage of metastasis and secondary tumor formation.

Chemical Information

CAS. Nr. 2411771-95-2
Appearance Solid
Molecular Weight 524.59
Formel C₂₉H₂₄N₄O₄S
Color Light yellow to light brown
SMILES

C=CC(NC1=CC(C)=CC(N2C(C=CC3=C2C4=C(N=C3)C=C(C=C4)C5=CC=C(C=C5)NS(C)(=O)=O)=O)=C1)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 20 mg/mL (38.13 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9063 mL

9.5313 mL

19.0625 mL

5 mM

0.3813 mL

1.9063 mL

3.8125 mL

10 mM

0.1906 mL

0.9531 mL

1.9063 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Sousa B B, et al. Selective Inhibition of Bruton’s Tyrosine Kinase by a Designed Covalent Ligand Leads to Potent Therapeutic Efficacy in Blood Cancers Relative to Clinically Used Inhibitors[J]. ACS Pharmacology & Translational Science, 2022.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9063 mL	9.5313 mL	19.0625 mL	47.6563 mL
	5 mM	0.3813 mL	1.9063 mL	3.8125 mL	9.5313 mL
	10 mM	0.1906 mL	0.9531 mL	1.9063 mL	4.7656 mL
	15 mM	0.1271 mL	0.6354 mL	1.2708 mL	3.1771 mL
	20 mM	0.0953 mL	0.4766 mL	0.9531 mL	2.3828 mL
	25 mM	0.0763 mL	0.3813 mL	0.7625 mL	1.9063 mL
	30 mM	0.0635 mL	0.3177 mL	0.6354 mL	1.5885 mL

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JS25

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Covalent Screening Library

Anti-Blood Cancer Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

JS25

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Covalent Screening Library

Anti-Blood Cancer Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

JS25 Related Classifications

HY-151808 Related Classifications