BTK

PCI-32765 is an orally bioavailable small-molecule inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity.

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).

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).

Zanubrutinib (BGB-3111) is a selective Bruton tyrosine kinase (BTK) inhibitor.

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.

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.

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.

Tirabrutinib (ONO-4059) is a highly selective, orally bioavailable BTK inhibitor with an IC50 of 2.2 nM.

GDC-0834 is a potent and selective BTK inhibitor.

(R)-Zanubrutinib is the R enantiomer of Zanubrutinib. Zanubrutinib is a selective Bruton tyrosine kinase (BTK) inhibitor.

SJF620 is a PROTAC that targets Bruton's tyrosine kinase (Btk) for degradation through its ligands for Cereblon (CRBN). With a DC50 of 7.9 nM, SJF620 effectively recruits CRBN, facilitating selective protein degradation. This compound is primarily utilized in research applications focused on Btk-related signaling pathways and therapeutic development for B-cell malignancies.

NRX-0492 is an orally active PROTAC BTK degrader that promotes the ubiquitination and proteasomal degradation of Bruton's tyrosine kinase (BTK) with DC50 values as low as 0.2 nM. This compound effectively inhibits B cell receptor (BCR)-mediated signaling, transcriptional programs, and chemokine secretion, demonstrating significant antitumor activity against chronic lymphocytic leukemia. NRX-0492 comprises a BTK inhibitor, an E3 ligase ligand derived from Thalidomide, and a PROTAC linker, making it a valuable tool for studying BTK-related pathways and therapies.

GBD-9 is a dual-action degrader that targets both BTK and GSPT1 by recruiting the E3 ligase cereblon (CRBN). It acts as a PROTAC to promote BTK degradation and functions as a molecular glue to induce GSPT1 degradation. GBD-9 exhibits significant antiproliferative activity in cancer cells, making it a promising candidate for cancer research.

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.

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.

NX-5948 (BTK-IN-24) is an orally bioavailable, blood-brain barrier-penetrant PROTAC degrader targeting Bruton's tyrosine kinase (BTK). It induces BTK degradation via the cereblon E3 ligase pathway, effectively inhibiting B cell activation. NX-5948 exhibits both anti-inflammatory and antitumor activities, supporting its use in cancer and immune-related research.

Zelebrudomide (NX-2127) is a novel, potent BTK degrader that induces proteasomal degradation through targeted ubiquitination, rather than direct inhibition. In addition to degrading BTK, Zelebrudomide (NX-2127) enhances immune responses by stimulating T cell activation and increasing IL-2 production in primary human T cells, supporting its potential in cancer and immunotherapy research.

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.

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.

XMU-MP-3 is a potent non-covalent inhibitor of Bruton's tyrosine kinase (BTK), exhibiting IC50 values of 10.7 nM for wild-type BTK and 17.0 nM for the C481S mutation in the presence of 10 μM ATP. This compound is known to induce apoptosis in BTK-dependent cells, making it a valuable tool for investigating B-cell receptor signaling and related pathways. XMU-MP-3 is applicable in research focused on hematological malignancies and immune responses.

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.

(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.

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.

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.

GDC-0834 Racemate is a potent and selective inhibitor of Bruton's tyrosine kinase (BTK), investigated as a potential treatment for rheumatoid arthritis.

AVL-292 is a highly selective, covalent Btk inhibitor.

CNX-774 is a potent Btk inhibitor (IC50 < 1 nM)

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).

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.

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.

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.

QL47 is a potent, selective and irreversible BTK kinase inhibitor with IC50 of 7 nM.

GDC0853 is a potent and orally BTK inhibitor.

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.

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.

PRN1008 is a reversible covalent, selective and oral active inhibitor of Bruton??s Tyrosine Kinase (BTK), with an IC50 of 1.3 nM.

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.

(±)-Zanubrutinib is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor.

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.