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BTK

Bruton's tyrosine kinase (abbreviated Btk or BTK), also known as tyrosine-protein kinase BTK, is a tyrosine kinase that is encoded by the BTK gene in humans. BTK plays a crucial role in B cell development.

  • Remibrutinib
    T167301787294-07-8
    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.
    • $98
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  • Sunvozertinib
    T641242370013-12-8
    Sunvozertinib (DZD9008) is a potent ErbBs and BTK inhibitor, with inhibitory effects on EGFR, Her2, and mutant epidermal growth factor. Sunvozertinib (DZD9008) showed inhibitory effects on EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, as well as Her2 exon 20 YVMA and EGFR WT A431 with IC50 of 20.4, 20.4, 1.1, 7.5, and 80.4 nM.
    • $30
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  • Tirabrutinib hydrochloride
    T123111439901-97-9
    Tirabrutinib hydrochloride is a potent, highly selective, and irreversible oral BTK inhibitor. Tirabrutinib hydrochloride irreversibly covalently binds to Bruton tyrosine kinase (BTK) in B cells and exhibits potent in vitro cytotoxicity against many types of B cell malignancies, as well as in vivo antitumor activity in mouse models [1].
    • $30
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  • zanubrutinib
    T75841691249-45-2
    Zanubrutinib (BGB-3111) is an inhibitor of Bruton tyrosine kinase (BTK).
    • $57
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  • evobrutinib
    T43871415823-73-2
    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.
    • $35
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  • Ibrutinib
    T1835936563-96-1
    Ibrutinib (PCI-32765) is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.
    • $36
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  • Edralbrutinib
    T632721858206-58-2In house
    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.
    • $197
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  • Rilzabrutinib
    T125421575596-29-0
    Rilzabrutinib (PRN1008) is a reversible covalent, selective, and orally active inhibitor of Bruton’s Tyrosine Kinase (BTK) with an IC50 of 1.3 nM.
    • $100
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  • BMS-986142
    T51381643368-58-4
    BMS-986142 is a potent and highly selective reversible BTK inhibitor (IC50: 0.5 nM).
    • $143
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  • Tolebrutinib
    T91251971920-73-6
    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).
    • $106
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  • Pirtobrutinib
    T362872101700-15-4
    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.
    • $31
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  • Orelabrutinib
    T123171655504-04-3
    Orelabrutinib (ICP-022) is an orally active and irreversible inhibitor of Bruton's tyrosine kinase (BTK).
    • $83
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  • AS-1763
    T397072227211-00-7
    AS-1763 is an orally available and selective BTK inhibitor with an IC50 of 0.85 nM.
    • $233
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  • ONO-4059 analog
    T69211351635-67-0
    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.
    • $38
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  • NX-2127
    T734632416131-46-7
    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.
    • $109
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  • XMU-MP-2
    T699802031152-10-8In house
    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.
    • $195
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  • BGB-8035
    T733812283349-24-4
    BGB-8035 is an orally available, selective and potent BTK inhibitor with antitumor activity that inhibits BTK, TEC and EGFR.BGB-8035 is used in the study of tumors and autoimmune diseases.
    • $413
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  • Branebrutinib
    T54071912445-55-6
    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).
    • $54
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  • Larotinib
    T733341438072-11-7
    Larotinib is an orally active, potent, and broad-spectrum tyrosine kinase inhibitor (TKI) with an IC50 of 0.6 nM for EGFR.
    • $74
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  • Acalabrutinib
    T36261420477-60-6
    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.
    • $39
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  • QL-X-138
    T389601469988-63-3In house
    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.
    • $193
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  • Btk inhibitor 2
    T106291558036-85-3
    Btk Inhibitor 2 (BGB-3111 analog) is a BTK inhibitor.
    • $31
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  • Saracatinib
    T6078379231-04-6
    Saracatinib (AZD0530) (AZD0530) is an effective Src inhibitor (IC50: 2.7 nM), and effective to Lck, Fyn, Lyn, Blk, Fgr and c-Yes.
    • $59
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  • Vecabrutinib
    T172201510829-06-7
    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.
    • $79
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  • TAK-020
    T95291627603-21-7
    TAK-020 is a potent covalent inhibitor of Btk with potential antitumor activity for the study of rheumatoid arthritis and immune-related diseases.
    • $148
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  • BIIB068
    T91921798787-27-5
    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.
    • $40
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  • CP-547632
    T10870L252003-65-9In house
    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.
    • $30
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  • MT-802
    T161572231744-29-7
    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).
    • $88
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  • AZ7550
    T135641421373-99-0
    AZ7550, an active metabolite of AZD9291, inhibits the activity of IGF1R (IC50: 1.6 μM).
    • $133
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  • RN486
    T19761242156-23-5
    RN486 is an effective and specific BTK inhibitor (IC50: 4 nM).
    • $77
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  • Fenebrutinib
    TQ02421434048-34-6
    Fenebrutinib (GDC-0853) is a selective and noncovalent inhibitor of Bruton’s tyrosine kinase (Btk) with a Ki of 0.91 nM.
    • $36
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  • QL47
    T167021469988-75-7
    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.
    • $85
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  • Spebrutinib
    T26031202757-89-8
    Spebrutinib (LMK-435) is an orally bioavailable, selective inhibitor of Bruton's agammaglobulinemia tyrosine kinase (BTK), with potential antineoplastic activity.
    • $35
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  • (±)-Zanubrutinib
    TQ00391633350-06-7
    (±)-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.
    • $42
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  • Tilfrinib
    T170981600515-49-8
    Tilfrinib is an effective and selective inhibitor of breast tumor kinase(Brk, IC50 = 3.15 nM) which displays anti-proliferative and anti-tumor activities.
    • $38
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  • CGI-1746
    T2472910232-84-7
    CGI1746 is a potent and highly selective small-molecule Btk inhibitor with IC50 of 1.9 nM.
    • $34
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  • QL-X-138 HCl
    T38960L In house
    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.
    • $195
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  • Avitinib
    T30241557267-42-1
    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.
    • $41
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  • N-piperidine Ibrutinib hydrochloride
    T121522231747-18-3
    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.
    • $48
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  • CNX-774
    T23021202759-32-7
    CNX-774 is a highly specific, irreversible, and orally active BTK inhibitor (IC50<1 nM).
    • $34
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  • Olmutinib
    T69181353550-13-6
    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.
    • $33
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  • Tirabrutinib
    TQ02361351636-18-4
    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.
    • $39
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  • BMX-IN-1
    T146921431525-23-3
    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.
    • $29
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  • CHMFL-BMX-078
    T42681808288-51-8
    CHMFL-BMX-078 is a highly potent and selective type II irreversible inhibitor of BMX kinase, with an IC50 of 11 nM.
    • $64
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  • BTK inhibitor 1
    T353302230724-66-8In house
    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.
    • $97
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  • BTK IN-1
    TQ02301270014-40-8
    BTK IN-1 [SNS062 analog] is an effective BTK inhibitor with an IC50 of less than 100 nM.
    • $32
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  • ARQ 531
    T143232095393-15-8
    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.
    • $51
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  • PCI 29732
    T4337330786-25-9
    PCI 29732 is a selective and irreversible Btk inhibitor with IC50 of 8.2 nM in a FRET based biochemical enzymology assay.
    • $30
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  • Tuxobertinib
    T90722414572-47-5
    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.
    • $33
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  • Ibrutinib deacryloylpiperidine
    T8636330786-24-8
    Ibrutinib deacryloylpiperidine (IBT4A) is a highly selective Bruton’s tyrosine kinase (BTK) irreversible inhibitor with an IC50 of 0.5 nM.
    • $33
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