BTK

Remibrutinib inhibits BTK activity with an IC50 value of 0.023 μM in blood. Remibrutinib is an effective and orally active Bruton tyrosine kinase inhibitor (IC50: 1 nM). Remibrutinib has the potential for Chronic urticaria (CU) treatment.

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

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

Zanubrutinib (BGB-3111) is an inhibitor of Bruton tyrosine kinase (BTK).

Evobrutinib(M2951) , also known as M-2951 and MSC-2364447C, is a highly selective inhibitor of the Bruton's tyrosine kinase (BTK), which is important in the development and functioning of various immune cells including B -lymphocytes and macrophages. PreClinical research suggests it may be therapeutically useful in certain autoimmune diseases.

Edralbrutinib (TG-1701) is a potent BTK inhibitor with anticancer activity used in treating tumors, immune system disorders, and blood and lymphatic system disorders. Additionally, Edralbrutinib is studied for its efficacy in membranous glomerulonephritis and optic neuromyelitis optica.

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

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

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

Pirtobrutinib (LOXO-305) is an advanced BTK inhibitor that displays high selectivity and operates through a non-covalent mechanism. This compound effectively inhibits various BTK C481 substitution mutations, leading to tumor regression in BTK-dependent lymphoma tumors in mouse xenograft models. Furthermore, Pirtobrutinib exhibits remarkable selectivity for BTK, with more than a 300-fold difference compared to 370 other kinases tested. Notably, at a concentration of 1 μM, Pirtobrutinib demonstrates no significant inhibition of non-kinase off-targets.

Tolebrutinib (PRN2246) is a potent, selective, orally active and brain-penetrant Bruton tyrosine kinase (BTK) inhibitor(IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively). It exhibits efficacy in central nervous system immunity. Tolebrutinib can be used for the research of multiple sclerosis (MS).

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

ONO-4059 analog (ONO-WG-307)ue is an analogue of ONO-4059, which is a highly potent and selective oral BTK inhibitor with IC50 of 23.9 nM. Phase 1.

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.

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.

Branebrutinib (BMS986195) is a potent, covalent inhibitor of Bruton's tyrosine kinase (BTK), >5,000-fold selective over all kinases outside of the Tec family (IC50 <1 nM for BTK).

Btk Inhibitor 2 (BGB-3111 analog) is a BTK inhibitor.

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.

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

Vecabrutinib (SNS-062) is a potent, noncovalent inhibitor of BTK (Kd: 0.3 nM) and ITK (Kd: 2.2 nM), with an IC50 of 24 nM for ITK.

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

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 IC50 values of QL-X-138 are 9.4 nM for BTK, 107.4 nM for MNK1, 26 nM for MNK2, and 3.5 μM against Dengue 2. QL-X-138 is used in the study of B-cell malignancies and B-cell malignant tumors.

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.

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.

AZ7550, an active metabolite of AZD9291, inhibits the activity of IGF1R (IC50: 1.6 μM).

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

Fenebrutinib (GDC-0853) is a selective and noncovalent inhibitor of Bruton’s tyrosine kinase (Btk) with a Ki of 0.91 nM.

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.

QL47 is a host-targeted small molecule antiviral agent with antiviral activity against dengue and other RNA viruses.QL47 acts as an inhibitor of viral translation and a covalent inhibitor of BTK, and can be used in the study of lymphomas.

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

(±)-Zanubrutinib ((±)-BGB-3111) is a potent, orally available Bruton's tyrosine kinase (Btk) inhibitor, exhibiting superior oral bioavailability, higher exposure, and more complete target inhibition.

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

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

N-piperidine Ibrutinib hydrochloride is a potent BTK inhibitor, a BTK ligand, inhibits WT BTK and C481S BTK, which can be used to synthesize a range of PROTAC molecules.N-piperidine Ibrutinib hydrochloride has potential anticancer N-piperidine Ibrutinib hydrochloride has potential anticancer activity, inhibiting the growth and proliferation of cancer cells.

CNX-774 is a highly specific, irreversible, and orally active BTK inhibitor (IC50<1 nM).

Tirabrutinib (GS-4059) (ONO-4059) is an orally active Bruton’s Tyrosine Kinase (Btk) inhibitor (can cross the blood-brain barrier (BBB)), with an IC50 of 6.8 nM. Tirabrutinib irreversibly and covalently binds to Btk and inhibits aberrant B cell receptor signaling. Tirabrutinib can be used in studies of autoimmune diseases and hematological malignancies.

BMX-IN-1 (BMX kinase inhibitor) is a selective inhibitor of bone marrow tyrosine kinase on chromosome X (BMX, IC50 = 8 nM) and the related Bruton’s tyrosine kinase (BTK, IC50 = 10.4 nM), but BMX-IN-1 is more than 47-656 fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity.

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.

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

ARQ-531 is a potent and orally active BTK inhibitor with potential antineoplastic activity, with IC50s of 0.85 nM and 0.39 nM for WT-BTK and C481S-BTK, respectively.

Olmutinib (HM61713, BI 1482694) is an orally available small molecule, a mutant-selective inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Olmutinib binds to and inhibits mutant forms of EGFR, thereby leading to cell death of EGFR-expressing tumor cells. As this agent is selective towards mutant forms of EGFR, its toxicity profile may be reduced as compared to non-selective EGFR inhibitors which also inhibit the EGFR wild-type form.

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

BTK IN-1 [SNS062 analog] is an effective BTK inhibitor with an IC50 of less than 100 nM.

Tilfrinib is an effective and selective inhibitor of breast tumor kinase(Brk, IC50 = 3.15 nM) which displays anti-proliferative and anti-tumor activities.

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

Ibrutinib deacryloylpiperidine (IBT4A) is a highly selective Bruton’s tyrosine kinase (BTK) irreversible inhibitor with an IC50 of 0.5 nM.

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

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.

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.

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.