- Cat. No.
- A11020
Ibrutinib (PCI-32765)
Synonyms: PCI-32765
PCI-32765 is an orally bioavailable small-molecule inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity.
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Bruton's tyrosine kinase (BTK) inhibitors act on a cytoplasmic kinase that relays signals from the B cell receptor. In 1993 two groups linked defects in the BTK gene to X-linked agammaglobulinemia, in which mature B cells fail to develop. BTK belongs to the Tec kinase family and is also expressed in myeloid cells such as macrophages and mast cells. Ibrutinib, first described as PCI-32765, binds covalently to a cysteine in the BTK active site and blocks B cell activation. Spebrutinib, listed as AVL-292 and as spebrutinib besylate, is another covalent inhibitor, while CGI1746 and RN486 bind reversibly. Ibrutinib-biotin and the fluorescent analog PCI-33380 serve as probes for BTK active-site occupancy.
Synonyms: PCI-32765
PCI-32765 is an orally bioavailable small-molecule inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity.
CGI1746 is a small-molecule Btk inhibitor chemotype with a new binding mode that stabilizes an inactive nonphosphorylated enzyme conformation.
Ibrutinib-biotin is a probe that consists of Ibrutinib linked to biotin via a long chain linker, extracted from patent WO2014059368A1 Compound 1-5, has an IC50 of 0.755-1.02 nM for BTK.
PCI-33380 is an irreversible Bruton's Tyrosine Kinase (BTK) inhibitor (fluorescent probe).
Synonyms: RN-486,RN 486
RN486 is a Bruton's tyrosine kinase (Btk) inhibitor.
CHMFL-BTK-01 (compound 9) is a highly selective irreversible BTK inhibitor, with an IC50 of 7 nM. CHMFL-BTK-01 (compound 9) potently inhibited BTK Y223 auto-phosphorylation.
Synonyms: GDC0834
GDC-0834 Racemate is a potent and selective inhibitor of Bruton's tyrosine kinase (BTK), investigated as a potential treatment for rheumatoid arthritis.
Synonyms: CC292
AVL-292 is a highly selective, covalent Btk inhibitor.
Synonyms: AVL292 benzenesulfonate
AVL-292 benzenesulfonate is a covalent, highly selective, orally active small molecule inhibitor of Btk with IC50 value of 0.5 nM, >1400-fold selectivity over the other kinases assayed.
Synonyms: GS 4059
ONO-4059 is a highly potent and selective oral BTK inhibitor
Synonyms: ACP196
ACP-196 is an orally available inhibitor of Bruton–s tyrosine kinase (BTK) with potential antineoplastic activity. It inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway.
Synonyms: HM 61713; BI-1482694
Olmutinib is a potent small molecule inhibitor of Bruton's tyrosine kinase (BTK).
(Rac)-IBT6A is a pyrazolo[3,4-d]pyrimidine derivative as a Btk kinase inhibitor.
Synonyms: LFM A13
LFM-A13 is a potent and selective inhibitor of Btk with IC50 of 17.2 uM; also inhibits PLK3 with IC50 of 7.2 uM.
PCI 29732 is a selective and irreversible Btk inhibitor with IC50 of 8.2 nM in a FRET based biochemical enzymology assay.
Synonyms: BTK Inhibitor
QL47 is a potent, selective and irreversible BTK kinase inhibitor with IC50 of 7 nM.
Synonyms: M-2951; MSC-2364447C
Evobrutinib is a highly selective BTK inhibitor with an IC50 of 37.9 nM. It has potential anti-neoplastic activity.
BMS-935177 a potent BTK inhibitor with improved kinase selectivity and superior oral exposure in multiple species. should provide useful clinical efficacy in autoimmune diseases.
Btk inhibitor 2 is a Bruton's tyrosine kinase (BTK) inhibitor.
Synonyms: SNS-062; FP-182; BSK-4841; BIIB-062
Vecabrutinib is a potent, noncovalent, reversible BTK inhibitor that inhibits signaling through the BCR pathway.
Synonyms: PCI-32765 (Racemate); PCI 32765
Ibrutinib Racemate (PCI-32765 Racemate) is the racemate of Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor with IC50 value of 0.5 nM.
MT-802 is a potent BTK degrader based on PROTAC technology, with a DC50 of 1 nM. MT-802 has potential to treat C481S mutant chronic lymphocytic leukemia (CLL).
PF-06250112 is a potent, highly selective, orally bioavailable BTK inhibitor with an IC50 of 0.5 nM, shows inhibitory effect toward BMX nonreceptor tyrosine kinase and TEC with IC50s of 0.9 nM and 1.2 nM, respectively.