2. Protein Tyrosine Kinase/RTK Apoptosis Epigenetics Cell Cycle/DNA Damage
  3. Btk Caspase Apoptosis PARP
  4. 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.

For research use only. We do not sell to patients.

BTK-IN-47

BTK-IN-47 Chemical Structure

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BTK-IN-47 Related Antibodies

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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Description

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[1].

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.

BTK-IN-47 Related Antibodies

Cell Proliferation Assay[1]

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).

Apoptosis Analysis[1]

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

BTK-IN-47 (15-30 mg/kg; injection; once daily; for 14 consecutive days) exhibits dose-dependent in vivo antitumor efficacy against Ramos cell xenografts, while inhibiting the BTK signaling pathway[1].

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.
Molecular Weight

490.56

Formula

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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BTK-IN-47 Related Classifications

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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:

BTK-IN-47BtkCaspaseApoptosisPARPBruton tyrosine kinasepoly ADP ribose polymeraseRamos cell xenograft modelG0/G1 phase cell cycle arrestBTK-C481S mutant cellsB-cell receptor signaling pathwayhematological tumor cell linesBALB/c nude miceBruton's tyrosine kinaseBTK Cys481caspase-dependent apoptotic pathwaySprague-Dawley ratsInhibitorinhibitorinhibit

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