For research use only. Not for therapeutic Use.
PF-4878691（Cat No.:I008711）is an investigational small molecule developed by Pfizer, designed to target and inhibit the activity of Bruton’s tyrosine kinase (BTK). BTK is a key enzyme in the B-cell receptor signaling pathway, which plays a critical role in the activation and proliferation of B-cells. Inhibition of BTK has therapeutic potential for treating various B-cell malignancies, such as chronic lymphocytic leukemia (CLL) and non-Hodgkin lymphoma (NHL). PF-4878691 is being explored in preclinical and early-phase clinical trials to evaluate its efficacy, safety, and potential as a targeted therapy for B-cell-related cancers.
| Catalog Number | I008711 |
| CAS Number | 532959-63-0 |
| Synonyms | 3M-852A; 852A; IMDZQ; PF-04878691; PF-4878691; S-32865; 3M852A; PF-04878691; PF4878691;S32865; 3M 852A; PF 04878691; PF 4878691; S 32865;N-(4-(4-amino-2-ethyl-1H-imidazo[4,5-c]quinolin-1-yl)butyl)methanesulfonamide |
| Molecular Formula | C17H23N5O2S |
| Purity | ≥95% |
| Target | Apoptosis |
| Solubility | Soluble in DMSO |
| Storage | Store at -20°C |
| IUPAC Name | N-[4-(4-amino-2-ethylimidazo[4,5-c]quinolin-1-yl)butyl]methanesulfonamide |
| InChI | InChI=1S/C17H23N5O2S/c1-3-14-21-15-16(12-8-4-5-9-13(12)20-17(15)18)22(14)11-7-6-10-19-25(2,23)24/h4-5,8-9,19H,3,6-7,10-11H2,1-2H3,(H2,18,20) |
| InChIKey | YZOQZEXYFLXNKA-UHFFFAOYSA-N |
| SMILES | CCC1=NC2=C(N1CCCCNS(=O)(=O)C)C3=CC=CC=C3N=C2N |
| Reference | 1:Clin Pharmacol Ther. 2011 Jun;89(6):821-9. doi: 10.1038/clpt.2011.60. Epub 2011 Mar 30. The innate immune response, clinical outcomes, and ex vivo HCV antiviral efficacy of a TLR7 agonist (PF-4878691).Fidock MD,Souberbielle BE,Laxton C,Rawal J,Delpuech-Adams O,Corey TP,Colman P,Kumar V,Cheng JB,Wright K,Srinivasan S,Rana K,Craig C,Horscroft N,Perros M,Westby M,Webster R,van der Ryst E, PMID: 21451504 DOI: 10.1038/clpt.2011.60 </br><span>Abstract:</span> Hepatitis C virus (HCV) infection is an issue of global concern, and studies are ongoing to identify new therapies that are both effective and safe. PF-4878691 is a Toll-like receptor 7 (TLR7) agonist modeled so as to dissociate its antiviral activities from its inflammatory activities. In a proof-of-mechanism study in healthy volunteers who received doses of 3, 6, and 9 mg of PF-4878691 twice a week for 2 weeks, PF-4878691 induced biomarkers of the immune and interferon (IFN) responses in a dose-dependent and dose-frequency-related manner. A novel finding was induction of TLR7 expression in vivo in response to PF-4878691, leading to an amplified biomarker response. A nonresponder at the 9-mg dose had a polymorphism in the IFN-α receptor 1 subunit (Val168Leu). Two subjects who had received 9-mg doses experienced serious adverse events (SAEs), characterized by flu-like symptoms, hypotension, and lymphopenia, leading to early termination of the study. TLR7 stimulation results in a pharmacologic response at levels commensurate with predicted antiviral efficacy, but these doses are associated with SAEs, raising concerns about the therapeutic window of this class of compounds for the treatment of HCV infection. |
