BTK

Tirabrutinib hydrochloride (GS-4059 (hydrochloride)) is a selective and novelBTK with IC50 2.2 nm inhibitor.

Sunvozertinib (DZD9008) is a potent ErbBs and BTK inhibitor and has inhibitory effects on EGFR, Her2 and mutant epidermal growth factor. Sunvozertinib showed inhibition of EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutation, and Her2 exon 20 YVMA and EGFR WT A431. IC50 were 20.4, 20.4, 1.1, 7.5 and 80.4 nM, respectively.

Ibrutinib (PCI-32765) is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.

IBT6A is an impurity of Ibrutinib. Ibrutinib is a Btk inhibitor (IC50: 0.5 nM). IBT6A can be used in the synthesis of IBT6A Ibrutinib dimer and IBT6A adduct.

CP-547632 is an orally available and potent, ATP-competitive dual inhibitor of VEGFR-2 and FGF kinase F with IC50s of 11 nM and 9 nM, respectively. CP-547632 is selective, with higher selectivity for VEGFR2 and bFGF than for EGFR, PDGFRβ and related tyrosine kinases (TKs). PDGFRβ and related tyrosine kinases (TKs) CP-547632 has antitumour activity.

BTK-IN-16 is a potential inhibitor of wild-type BTK and C481S mutants.BTK-IN-16 can be used to study various autoimmune diseases and cancers caused by BTK.

Edralbrutinib (TG-1701) is a potent BTK inhibitor with anticancer activity and is used in the treatment of tumors, immune system disorders, and blood and lymphatic system disorders.Edralbrutinib is used in the study of membranous glomerulonephritis and optic neuromyelitis optica.

Acalabrutinib enantiomer (R-Acalabrutinib) is a chemical compound that belongs to the class of Bruton’s tyrosine kinase (BTK) inhibitors. Acarabitinib enantiomers can be used in the study of cancer, autoimmune diseases and chronic inflammation.

Larotinib is an orally active, potent, and broad-spectrum tyrosine kinase inhibitor (TKI) with an IC50 of 0.6 nM for EGFR.

N-piperidine Ibrutinib is a potent BTK inhibitor with IC50s of 51.0 for WT BTK and 30.7 nM for C481S BTK respectively. N-piperidine Ibrutinib can be used as a BTK ligand in the synthesis of a series of PROTACs, such as SJF620. SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM.

XMU-MP-2 is a potent and selective protease inhibitor with anticancer activity that inhibits the growth of oncogenic BRK-driven tumors in a mouse xenograft model.

QL-X-138 HCl is a novel selective and highly potent BTK/MNK dual-kinase inhibitor with anticancer activity that binds covalently to BTK and noncovalently to MNK. QL-X-138 HCl inhibited BTK, MNK1, and MNK2 kinases. QL-X-138 HCl has anti-dengue virus 2 activity and shows anti-proliferative activity in acute myeloid leukemia cells. QL-X-138 HCl can be used to study lymphoma and leukemia.

BTK inhibitor 1 (Compound 27) is a BTK inhibitor (IC50: 0.11 nM) with an inhibitory effect on B-cell activation in hWB with an IC50 of 2 nM.

JAK3/ BTk-in-1 is a dual JAK3/BTK inhibitor that specifically targets and inhibits Janus kinase 3 (JAK3) and Bruton's tyrosine kinase (BTK), two important targets in autoimmune diseases. JAK3/ BTk-in-1 simultaneously inhibited the BTK/JAK3 signaling pathway, showing a synergistic effect. JAK3/ BTK-in-1 is a potential compound for the treatment of immune-related diseases, such as autoimmune diseases, certain types of cancer (including lymphoma and leukemia), and other diseases that may be characterized by an unbalanced immune response.

ACP-5862 is a major active and pyrrolidine ring-opened metabolite of Acalabrutinib (IC50: 5.0 nM for BTK). Acalabrutinib is an irreversible and highly selective BTK inhibitor (IC50: 3 nM; EC50: 8 nM).

JAK3/ BTk-in-2 is a potent JAK3/BTK inhibitor. JAK3/ BTk-in-2 inhibits both BTK and JAK3, which are two important targets IN autoimmune diseases. JAK3/ BTk-in-2 simultaneously inhibits the BTK/JAK3 signaling pathway, showing a synergistic effect. JAK3/ BTk-in-2 has the potential to treat diseases associated with abnormal JAK3 and BTK activity.

QL-X-138 is a potent and selective BTK and MNK dual kinase inhibitor that binds covalently to BTK and non-covalently to MNK.The IC 50 s of QL-X-138 against BTK, MNK1 and MNK2 kinases are 9.4 nM, 107.4 nM and 26 nM, respectively.The IC 50 s of QL-X-138 against Dengue 2 is 3.5 μM.QL-X-138 is used in the study of B-cell malignancies. QL-X-138 inhibits dengue virus 2 with an IC 50 of 3.5 μM. QL-X-138 can be used in the study of B-cell malignant tumors.

RN486 is an effective and specific BTK inhibitor (IC50: 4 nM).

Saracatinib (AZD0530) (AZD0530) is an effective Src inhibitor (IC50: 2.7 nM), and effective to Lck, Fyn, Lyn, Blk, Fgr and c-Yes.

BIIB068 is an selective, reversible and orally active BTK inhibitor (IC50 = 1 nM, Kd = 0.3 nM). BIIB068 is 400 times more selective for BTK than other kinases.

LFM-A13（IC50=2.5 μM）, a specific Bruton's tyrosine kinase (BTK), is more than 100-fold specificity than other protein kinases, such as JAK1, JAK2, HCK, EGFR, and IRK.

BLK degrader 1 is a selective B lymphoid tyrosine kinase (BLK) degrader with anticancer activity and can be used for cancer research.

BTK inhibitor 17 is a potent irreversible BTK inhibitor (IC50 = 2.1 nM). BTK inhibitor 17 can be used in rheumatoid arthritis studies.

BTK IN-1 (SNS062 analog) (SNS062 analog) is an effective BTK inhibitor (IC50: <100 nM).

JDB175, a selective BTK inhibitor with oral bioavailability, demonstrates excellent penetration through the blood-brain barrier. It exhibits potent activity against central nervous system lymphoma in a mouse model, with no apparent toxicity. JDB175 effectively suppresses human lymphoma cell proliferation by inhibiting the BTK signaling pathway, induces cell cycle arrest, and promotes apoptosis[1].

MT-802 is an effective BTK degrader based on PROTAC technology (DC50: 1 nM). MT-802 has the potential to treat C481S mutant chronic lymphocytic leukemia (CLL).

(Rac)-IBT6A is the racemate of IBT6A. IBT6A is an impurity of ibrutinib and can be used in the synthesis of IBT6A ibrutinib dimers and IBT6A adducts. 3',4'-Dimerization of ibrutinib and ibrutinib dimers.

AS-1763 is an orally available and selective BTK inhibitor with an IC50 of 0.85 nM.

DBt-10 is a potent Bruton's tyrosine kinase (BTK) degrader [1].

PCI-33380 is an irreversible inhibitor of Bruton's Tyrosine Kinase.

PROTAC BTK Degrader-6 (Compound 15), with a DC50 of 3.18 nM, exhibits anti-inflammatory properties by inhibiting NF-κB activation and suppressing the expression of pro-inflammatory cytokines, such as IL-1β and IL-6 [1].

BTK-IN-25 (compound 71) is a potent BTK inhibitor, demonstrating an IC50 of 0.77 nM against BTK(C481S) and achieving an IC50 of 1 nM in DOHH2 cells [1].

Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that, upon phosphorylation, binds to immunoreceptor tyrosine-based activation motifs of FcRγ chains and mediates downstream signaling related to platelet function and inflammation. Syk inhibit

Avitinib (AC0010), also known as AC0010 or AC0010MA, is an orally available, irreversible, epidermal growth factor receptor (EGFR) mutant-selective inhibitor, with potential antineoplastic activity. Upon oral administration, avitinib covalently binds to and inhibits the activity of mutant forms of EGFR, including the drug-resistant T790M EGFR mutant, which prevents signaling mediated by mutant forms of EGFR. This may both induce cell death and inhibit tumor growth in EGFR-mutated tumor cells. EGFR, a receptor tyrosine kinase that is mutated in a variety of Ys, plays a key role in tumor cell proliferation and tumor vascularization. As this agent is selective towards mutant forms of EGFR, its toxicity profile may be reduced when compared to non-selective EGFR inhibitors, which also inhibit wild-type EGFR.

Spebrutinib (LMK-435) is an orally bioavailable, selective inhibitor of Bruton's agammaglobulinemia tyrosine kinase (BTK), with potential antineoplastic activity.

NX-2127 (ETX2514 Triethylamine) is an orally active BTK inhibitor that induces degradation of mutant BTKC481S in cells.NX-2127 has potent antiproliferative activity and inhibits the proliferation of BTKC481S mutant TMD8 cells.NX-2127 potently catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) at 25 nM and 54 nM, respectively. NX-2127 is associated with the immune system, stimulating T cell activation and increasing IL-2 production in primary human T cells.

PCI 29732 is a selective and irreversible Btk inhibitor with IC50 of 8.2 nM in a FRET based biochemical enzymology assay.

BMS-986142 is a potent and highly selective reversible BTK inhibitor (IC50: 0.5 nM).

Orelabrutinib (ICP-022) is an orally active and irreversible inhibitor of Bruton's tyrosine kinase (BTK).

CHMFL-BMX-078 is a highly potent and selective type II irreversible BMX kinase inhibitor with an IC50 of 11 nM.

CGI1746 is a potent and highly selective small-molecule Btk inhibitor with IC50 of 1.9 nM.

BTK-IN-27 (example 8), a potent BTK inhibitor with an IC50 of 0.2 nM, demonstrates anti-proliferative effects in TMD8 cells with an IC50 of less than 5 nM. It is suitable for the research of various conditions including cancer, lymphoma, leukemia, and immunological diseases [1].

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

G-744 is a selective and orally active inhibitor of Btk (IC50: 2 nM). G-744 is well-tolerated, metabolically stable. It also has an efficacious to treat arthritis.

Fenebrutinib (GDC-0853) is a selective and noncovalent Btk inhibitor (Ki: 0.91 nM).

PF-06250112 is an effective and highly selective BTK inhibitor (IC50: 0.5 nM. PF-06250112 displays an inhibitory effect toward BMX nonreceptor tyrosine kinase and TEC (IC50s: 0.9 nM and 1.2 nM, respectively).

SB-633825 can inhibit cancer cell growth and angiogenesis. SB-633825 is an effective and ATP-competitive inhibitor of TIE2, LOK, and BRK (IC50s: 3.5 nM, 66 nM, 150 nM, respectively).

Acalabrutinib (ACP-196), also known as ACP-196, is an orally available inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity. Upon administration, ACP-196 inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and BTK-mediated activation of downstream survival pathways. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. BTK, a member of the src-related BTK/Tec family of cytoplasmic tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role in B lymphocyte development, activation, signaling, proliferation and survival.

Tuxobertinib (BDTX-189) is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations(KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively). BDTX-189 exhibits anticancer activity.

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