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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: CG-026806
CG-806 is an orally active, potent and non-covalent pan-FLT3/pan-BTK inhibitor with an IC50 of 0.08 μM for FLT3. CG-806 has an IC50 of 11 nM against FLT3 wild type (WT)-transfected Ba/F3 cells.
ARQ 531 is a reversible non-covalent inhibitor of Bruton’s Tyrosine Kinase (BTK), with IC50s of 0.85 nM and 0.39 nM for WT-BTK and C481S-BTK, respectively.
BMS-986142 is a potent and highly selective reversible inhibitor of Bruton's tyrosine kinase (BTK) with an IC50 of 0.5 nM.
Synonyms: PRN 1008
PRN1008 is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 1.3 nM.
Synonyms: BMS-986195
Branebrutinib (BMS-986195) is a highly potent, selective covalent, irreversible inhibitor of Bruton’s tyrosine kinase (BTK), with an IC50 of 0.1 nM.
G-744 is a highly potent, selective and orally active Btk inhibitor with an IC50 of 2 nM. G-744 is metabolically stable, well tolerated and efficacious to treat arthritis.
Synonyms: (±)-BGB-3111; BGB3111
(±)-Zanubrutinib is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor.
Synonyms: ONO-4059; GS-4059
Tirabrutinib (ONO-4059) is a highly selective, orally bioavailable BTK inhibitor with an IC50 of 2.2 nM.
Synonyms: (R)-BGB-3111; BGB3111
(R)-Zanubrutinib is the R enantiomer of Zanubrutinib. Zanubrutinib is a selective Bruton tyrosine kinase (BTK) inhibitor.
Synonyms: Ibrutinib analog
Btk inhibitor 1 R enantiomer (Ibrutinib analog) (Compound 14) is a covalent and irreversible Bruton’s tyrosine kinase (BTK) inhibitor and can be used in synthesis of Ibrutinib and ibrutinib-based activity-based probes (ABPs).
Synonyms: Ibrutinib analog hydrochloride
Btk inhibitor 1 R enantiomer hydrochloride (Ibrutinib analog hydrochloride) (Compound 14) is a covalent and irreversible Bruton’s tyrosine kinase (BTK) inhibitor and can be used in synthesis of Ibrutinib and ibrutinib-based activity-based probes (ABPs).
Synonyms: BGB-3111
Zanubrutinib (BGB-3111) is a selective Bruton tyrosine kinase (BTK) inhibitor.
Synonyms: ICP-022
Orelabrutinib (ICP-022) is a potent, orally active, and irreversible Bruton's tyrosine kinase (BTK) inhibitor with potential antineoplastic activity.
Remibrutinib, is a potent and orally active bruton tyrosine kinase (BTK) inhibitor with an IC50 value of 1 nM.
Synonyms: ONO-4059 hydrochloride; GS-4059 hydrochloride
Tirabrutinib (ONO-4059) hydrochloride is a selective and novel inhibitor of BTK with IC50 2.2 nm, Tirabrutinib binds to BTK within B cells, thereby preventing B-cell receptor signaling and impeding B-cell development.
Synonyms: Compound 27
BTK inhibitor 1 (compound 27) is an inhibitor of BTK with an IC50 of 0.11 nM for Btk and inhibits B cell activation in hWB with an IC50 of 2 nM.
Synonyms: DZD9008
Sunvozertinib (DZD9008) is a potent, orally active inhibitor of ErbB family kinases, including mutant forms of EGFR and HER2, as well as Bruton's tyrosine kinase (BTK). It demonstrates strong inhibitory activity against a range of clinically relevant EGFR mutations, with IC₅₀ values of 20.4 nM for EGFR exon 20 NPH insertion, 20.4 nM for EGFR exon 20 ASV insertion, 1.1 nM for EGFR L858R/T790M, and 7.5 nM for HER2 exon 20 YVMA mutation. It exhibits reduced activity against wild-type EGFR (IC₅₀ = 80.4 nM in A431 cells), supporting its selectivity for mutant forms. Sunvozertinib is being investigated as a targeted therapy for non-small cell lung cancers harboring EGFR or HER2 exon 20 alterations.
Synonyms: Abivertinib maleate; AC0010 maleate
Avitinib (Abivertinib) maleate is a third-generation, irreversible, and orally active selective EGFR inhibitor with IC50 values of 0.18 nM for both EGFR^L858R and EGFR^T790M, and 7.68 nM for wild-type EGFR. In addition to its EGFR-targeting activity, Avitinib maleate also inhibits BTK phosphorylation and induces apoptosis in mantle cell lymphoma models, demonstrating broad-spectrum anticancer efficacy.
PLS-123 is a covalent, irreversible inhibitor of Bruton's tyrosine kinase (BTK), displaying an IC50 of less than 5 nM. It effectively disrupts BTK's catalytic activity at Tyr551 and self-activation at Tyr223, leading to the inhibition of key signaling pathways, including AKT/mTOR and MAPK, as well as blocking PLCγ2 activation. PLS-123 exhibits potent anti-proliferative effects against a range of B-cell lymphoma cell lines, inducing apoptosis through a caspase-dependent mechanism. Additionally, it demonstrates substantial antitumor efficacy in the OCI-Ly7 xenograft model, making it a valuable tool for research in lymphoma.
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TL-895 is a potent, orally bioavailable, irreversible inhibitor of Bruton's tyrosine kinase (BTK) that functions as an ATP-competitive agent. It demonstrates high selectivity with an average IC50 of 1.5 nM against recombinant BTK and minimal activity against BLK, BMX, and TXK. TL-895 effectively inhibits BTK auto-phosphorylation at the Y223 site (IC50: 1-10 nM) and suppresses the production of inflammatory cytokines such as IL-8, IL-1β, MCP-1, and TNF-α in monocytes and macrophages. This compound is valuable for investigating chronic lymphocytic leukemia (CLL), myelofibrosis (MF), and various B-cell malignancies.
EGFR-IN-40 is a selective inhibitor targeting Bruton's tyrosine kinase (BTK), epidermal growth factor receptor (EGFR), and IL-2-inducible T-cell kinase (ITK). It exhibits potent inhibitory activity with IC50 values of 1.2 nM for BTK, 5.3 nM for EGFR, and 46.1 nM for ITK. This compound is valuable for research applications focusing on cancer therapeutics and signaling pathways related to these kinases.
Synonyms: (S)-DZD9008
(S)-Sunvozertinib, the S-enantiomer of Sunvozertinib, acts as a selective inhibitor of the ErbB family of receptors and Bruton's tyrosine kinase (BTK). It demonstrates potent inhibitory activity against multiple oncogenic variants of EGFR, including exon 20 insertions and the L858R/T790M mutation, with IC50 values of 51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively. Due to its dual action on both ErbBs and BTK, (S)-Sunvozertinib is poised for applications in targeted cancer therapy and research into mechanisms of resistance in EGFR-driven malignancies.
Synonyms: LP-168
Rocbrutinib is a highly selective Bruton's tyrosine kinase (BTK) inhibitor, exhibiting an IC50 of 0.11 nM for wild-type BTK and 1.0 nM for the C481S-mutated variant. It demonstrates significant anti-leukemic activity by reducing cell viability, inducing cytotoxic effects, and inhibiting cell migration. This compound is applicable in research surrounding chronic lymphocytic leukemia, non-Hodgkin's lymphoma, and mantle cell lymphoma.
Synonyms: CG-806
Luxeptinib is a first-in-class, non-covalent pan-FLT3 and pan-BTK inhibitor that exhibits potent oral activity. This compound effectively induces cell cycle arrest, apoptosis, or autophagy in acute myeloid leukemia cells, making it a significant tool for cancer research. Its dual-targeting mechanism positions Luxeptinib as a potential therapeutic candidate in the treatment of hematological malignancies.
