BTK-IN-52
BTK-IN-52 is a BTK inhibitor with an IC50 of 126.70 nM. BTK-IN-52 inhibits BTK phosphorylation, induces G0/G1 cell cycle arrest and apoptosis (apoptosis) in cancer cells, and inhibits cancer cell proliferation. BTK-IN-52 inhibits tumor growth in xenograft models. BTK-IN-52 inhibits off-target TEC and JAK2 kinases in selectivity assays. BTK-IN-52 can be used in research related to hematological diseases and lymphoma.
For research use only. We do not sell to patients.
- CAS No.: 3119675-75-8
- Formula: C26H22Cl2N4O4
- Molecular Weight:525.38
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| U-937 | IC50 |
0.89 μM
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Antiproliferative activity against human U-937 histiocytic lymphoma cells assessed as viability reduction incubated 48 hrs by CCK-8 assay.
Antiproliferative activity against human U-937 histiocytic lymphoma cells assessed as viability reduction incubated 48 hrs by CCK-8 assay.
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42566884 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U-937
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Concentration:0.3125, 0.625, 1.25, 2.5, and 5 μM
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Incubation Time:48 h
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Result:U-937 IC50 was 0.89 μM.
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Cell Line:U-937
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Concentration:1, 10, 100, and 1000 nM
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Incubation Time:48 h
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Result:Dose-dependently inhibited BTK phosphorylation at Tyr223 while total BTK remained unchanged.
The p-BTK/BTK ratio decreased from 100% in vehicle control to approximately 20% at 1000 nM.
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Cell Line:U-937
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Concentration:0.5, 0.75, and 1 μM
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Incubation Time:72 h
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Result:Induced G0/G1 phase arrest.
G1/G0 proportions were 59.5%, 55.3%, and 52.6% at 0.5, 0.75, and 1 μM, respectively; S-phase proportions were 36.7%, 36.0%, and 39.3%; G2/M proportions were 0%, 4.77%, and 0.47%.
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Cell Line:U-937
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Concentration:1, 5, and 10 μM
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Incubation Time:48 h
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Result:Apoptosis rates were 26.52%, 48.63%, and 58.48% at 1, 5, and 10 μM, respectively.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSG (NOD/SCID gamma, female, five-week-old)[1]
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Dosage:25 mg/kg; 50 mg/kg; 100 mg/kg
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Administration:i.p.; once every two days; seven administrations
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Result:Day 7 tumor luminescence flux was 16,237 cts at 25 mg/kg, 15,150 cts at 50 mg/kg, and 7,814 cts at 100 mg/kg.
Day 21 tumor luminescence flux was 341,871 cts at 25 mg/kg, 178,622 cts at 50 mg/kg, and 9,894 cts at 100 mg/kg.
Tumor growth inhibition was 20.2% at 25 mg/kg, 32.7% at 50 mg/kg, and 95.5% at 100 mg/kg.
- Somatic Cell Culture
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Apoptosis Solutions
- MTT Cell Proliferation Assay
- Western Blot
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- Patient-Derived Orthotopic Xenograft (PDOX)
- Protocol for Cell Cycle
- CCK-8/WST-8 Cell Proliferation Assay
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- Kinase activity and phosphorylation assays
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- Patient-Derived Xenograft (PDX)
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Protocol for Kinase activity and phosphorylation assays
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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CAS No. 3119675-75-8
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Molecular Weight 525.38
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Formula C26H22Cl2N4O4
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SMILES
O=C(NNC(CC1=CC=C(Cl)C=C1Cl)=O)C2=CC=C(NC3=CC=NC4=CC(OC)=C(OC)C=C34)C=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BTK-IN-52 Related Classifications
HY-190481 Related Classifications
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