BTK-IN-47
BTK-IN-47 (Compound 9e) is a covalent, selective BTK inhibitor with an IC50 of 5.15 nM against BTK. BTK-IN-47 inhibits the BTK signaling pathway, induces cell cycle arrest, and activates the canonical Caspase-dependent Apoptotic pathway (promoting the cleavage of Caspase-3, Caspase-7 and PARP), without inducing necroptosis, pyroptosis or ferroptosis. BTK-IN-47 exerts dose-dependent antiproliferative activity against hematologic tumor cell lines. BTK-IN-47 exhibits dose-dependent in vivo antitumor activity in a Ramos cell xenograft model in BALB/c nude mice. BTK-IN-47 can be used for the research of hematologic malignancies.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Formel: C28H26N8O
- Molecular Weight:490.56
-
Speicherung:
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]
-
Biologische Aktivität
-
Chemical Information
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
Alle Caspase Isoform-spezifische Produkte anzeigen
More
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
Caspase 3 |
Caspase-7 |
In Vitro
BTK-IN-47 (compound 9e) (serial dilutions; per Z'-Lyte protocol) potently inhibits recombinant human BTK kinase activity in vitro with an IC50 of 5.15 nM[1].
BTK-IN-47 (compound 9e) (serial dilutions; 48 h) inhibits the proliferation of Ramos, Raji, MOLM-13, and Jurkat hematological tumor cell lines in vitro with IC50 values ranging from 2.04 to 4.03 μM[1].
BTK-IN-47 (compound 9e) (1-10 μM; 48 h) induces G1 phase cell cycle arrest and caspase-mediated apoptosis in Ramos cells in vitro in a dose-dependent manner, without activating necroptotic, pyroptotic, or ferroptotic pathways[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Ramos, Raji, MOLM-13, Jurkat hematological tumor cell lines
-
Concentration:Serial dilutions
-
Incubation Time:48 h
-
Result:Exhibited antiproliferative activity with IC50 values of 2.68 ± 0.54 μM (Ramos), 2.04 ± 1.51 μM (Raji), 2.73 ± 0.17 μM (MOLM-13), and 4.03 ± 0.43 μM (Jurkat).
-
Cell Line:Ramos cells
-
Concentration:1-10 μM
-
Incubation Time:48 h
-
Result:Induced apoptosis with rates of 30.7% (1 μM) and 37.5% (10 μM), and facilitated cleavage of Caspase-3, Caspase-7, and PARP.
Parmacokinetics
| Species | Dose | Route | T1/2 | Cmax | AUC0-t | AUC0-∞ | Vz | CL | Bioavailability |
|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 1 mg/kg | i.v. | 9.75 ± 2.46 h | 41.82 ± 4.71 μg/L | 161.45 ± 59.89 μg/L·h | 190.46 ± 71.62 μg/L·h | 80.43 ± 36.64 L/kg | 5.70 ± 1.79 L/h/kg | / |
| Rat[1] | 10 mg/kg | p.o. | 2.74 ± 1.00 h | 87.31 ± 32.80 μg/L | 190.97 ± 19.36 μg/L·h | 192.74 ± 22.35 μg/L·h | 20.14 ± 4.96 L/kg | 5.23 ± 0.57 L/h/kg | 11.83 % |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BALB/c nude (female, 6 to 8 weeks old, subcutaneous xenograft of Ramos cells)[1]
-
Dosage:15 mg/kg/day; 30 mg/kg/day
-
Administration:injected; daily; 14 days
-
Result:Achieved 82.3% tumor growth inhibition rate and reduced Ki-67 labeling index to a level comparable to ibrutinib at 15 mg/kg/day.
Achieved 87.5% tumor growth inhibition rate, significantly reduced phosphorylation of BTK and PLCγ2 in tumor tissue, and lowered Ki-67 labeling index to 41.60% at 30 mg/kg/day.
Caused no significant body weight loss or systemic tissue damage at either dose.
Chemical Information
-
Molecular Weight 490.56
-
Formel C28H26N8O
-
SMILES
NC1=C2C(N([C@H]3CN(C4=NN=C(C=C)C=C4)CCC3)N=C2C5=CC=C(OC6=CC=CC=C6)C=C5)=NC=N1
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
BTK-IN-47 Related Classifications
HY-181996 Related Classifications
Powered by Bioz
Keywords
- BTK-IN-47
- Btk
- Caspase
- Apoptosis
- PARP
- Ramos cell xenograft model
- G0/G1 phase cell cycle arrest
- BTK-C481S mutant cells
- B-cell receptor signaling pathway
- hematological tumor cell lines
- BALB/c nude mice
- Bruton's tyrosine kinase
- BTK Cys481
- caspase-dependent apoptotic pathway
- Sprague-Dawley rats
- Inhibitor
- inhibitor
- inhibit