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PCI-32765, a selective, irreversible Btk inhibitor, is a novel, molecularly targeted agent for patients with B-cell malignancies, and is particularly active in patients with CLL. B-cell receptor (BCR) signaling is a critical pathway in the pathogenesis of several B-cell malignancies, including chronic lymphocytic leukemia (CLL), and can be targeted by inhibitors of BCR-associated kinases, such as Bruton tyrosine kinase (Btk). PCI-32765 significantly inhibited CLL cell survival, DNA synthesis, and migration in response to tissue homing chemokines (CXCL12, CXCL13). PCI-32765 also down-regulated secretion of BCR-dependent chemokines (CCL3, CCL4) by the CLL cells, both in vitro and in vivo. In an adoptive transfer TCL1 mouse model of CLL, PCI-32765 affected disease progression. In this model, PCI-32765 caused a transient early lymphocytosis, and profoundly inhibited CLL progression, as assessed by weight, development, and extent of hepatospenomegaly, and survival. Inhibition of BTK by PCI-32765 overcomes BCR- and chemokine-controlled integrin-mediated retention and homing of malignant B cells in their growth- and survival-supporting lymph node and bone marrow microenvironment, which results in clinically evident CLL regression.
Int Immunopharmacol. 2022 Dec;113(Pt B):109469.
Ibrutinib suppresses the activation of neutrophils and macrophages and exerts therapeutic effect on acute peritonitis induced by zymosan
PCI-32765 purchased from AbMole
BMC Biol. 2021 May 20;19(1):108.
Very long intergenic non-coding (vlinc) RNAs directly regulate multiple genes in cis and trans
PCI-32765 purchased from AbMole
J Virol. 2020 Feb 14;94(5):e01791-19.
Targeting Kaposi's Sarcoma-Associated Herpesvirus ORF21 Tyrosine Kinase and Viral Lytic Reactivation by Tyrosine Kinase Inhibitors Approved for Clinical Use
PCI-32765 purchased from AbMole
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Source | Blood (2011). Figure 3. PCI-32765 |
| Method | Western Bolt | |
| Cell Lines | CD19+ cells | |
| Concentrations | 10 μM | |
| Incubation Time | 8 h | |
| Results | We found that inhibition of caspase activity by z-VAD-fmk completely prevented the induction of apoptosis provided by PCI-32765 concurrent with a decrease in cleaved PARP expression and a decrease in enzymatic activity of caspase-3 |
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Source | Blood (2011). Figure 2. PCI-32765 |
| Method | MTT assay | |
| Cell Lines | CD19+ cells | |
| Concentrations | 10 μM | |
| Incubation Time | 12-72 h | |
| Results | We found that there were no significant differences in PCI-32765–induced cell death based on interphase cytogenetic analysis |
| Cell Experiment | |
|---|---|
| Cell lines | osteoblast cells |
| Preparation method | In vitro osteoblast differentiation Cells derived from calvaria were cultured in an osteogenic medium (50 μM ascorbic acid, 10 nM dexamethasone and 10 mM β- glycerophosphate) in the presence of ibrutinib and subjected to an analysis of the activity of alkaline phosphatase (after 7 days) and bone nodule formation (after 21 days). |
| Concentrations | 0~100nM |
| Incubation time | 7days |
| Animal Experiment | |
|---|---|
| Animal models | RANKL-induced bone loss in mice |
| Formulation | saline |
| Dosages | 6.25, 12.5 or 25 mg/kg 1 h before the first GST-RANKL injection |
| Administration | oral gavage |
| Molecular Weight | 440.5 |
| Formula | C25H24N6O2 |
| CAS Number | 936563-96-1 |
| Solubility (25°C) | DMSO ≥30 mg/mL |
| Storage | 2-8°C, protect from light, dry, sealed |
| Related BTK Products |
|---|
| Spebrutinib (AVL-292)
Spebrutinib (AVL-292) is an oral, potent and selective small molecule covalent inhibitor of Btk (IC50 < 0.5 nM). |
| CNX-774
CNX-774 is an irreversible, orally active, and highly selective BTK inhibitor with IC50 of <1 nM. |
| GDC-0834
GDC-0834 is a novel potent and selective BTK inhibitor with IC50 of 5.9 nM. |
| CGI1746
CGI1746 is a potent and highly selective small-molecule inhibitor of the Btk with IC50 of 1.9 nM. |
| RN486
RN486 is a Bruton's tyrosine kinase (Btk) inhibitor with an IC50 Value of 4.0 nM. |
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Products are for research use only. Not for human use. We do not sell to patients.
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