BTK
BTK Products
Catalog No. | Information | Product Use Citations | Product Validations |
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S2680 |
Ibrutinib (PCI-32765)Ibrutinib (PCI-32765) is a potent and highly selective Brutons tyrosine kinase (Btk) inhibitor with IC50 of 0.5 nM in cell-free assays, modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc. Ibrutinib is applicable as a Btk ligand in the synthesis of a series of PROTACs including P13I. |
![]() ![]() Identification of Btk as a potent kinase for WIP tyrosine phosphorylation. Total protein lysates were prepared from THP-1 cells that were stably transfected with wild-type WIP-EGFP and treated with PCI-32765 at the concentration specified on the blots for 2h before pervanadate treatment for 30 min. In all cases WIP-EGFP was immunoprecipitated from cell lysates using anti-EGFP antibody and membranes subsequently blotted with the pY (4G10) antibody, EGFP antibody and β-Tubulin.
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S7173 |
Spebrutinib (CC-292)Spebrutinib (CC-292, AVL-292) is a covalent, orally active, and highly selective BTK inhibitor with IC50 of <0.5 nM, displaying at least 1400-fold selectivity over the other kinases assayed. Phase 1. |
![]() ![]() Effects of AVL-292, CNX-774 and dasatinib on IgE-mediated histamine release in human basophils. Basophils (BA) obtained from three nonallergic donors (A). |
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S7257 |
CNX-774CNX-774 is an irreversible, orally active, and highly selective BTK inhibitor with IC50 of <1 nM. |
![]() ![]() Effects of AVL-292, CNX-774 and dasatinib on IgE-mediated histamine release in human basophils. Basophils (BA) obtained from three nonallergic donors (A), three patients allergic to Der p 2, and three patients allergic to Phl p 5 (B and C) were preincubated in control medium (Co) or medium containing various concentrations of AVL-292, CNX-774, or dasatinib (0.001-1 μmol/L) at 37°C for 30 minutes. Then, cells were exposed to anti-IgE antibody E-124.2.8 (1 μg/mL; nonallergic donors) or recombinant allergens (1 μg/mL of rDer p 2 or rPhl p 5 in allergic patients) at 37°C for 30 minutes. After centrifugation, histamine concentrations were determined in cell-free supernatants and cell lysates. Histamine release is expressed as percentage of total histamine. Results show the percentage of control and represent mean SD from three independent experiments (three donors). Asterisk (*): P<0.05 by Student's t test with Bonferroni correction |
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S8832 |
Branebrutinib (BMS-986195)Branebrutinib (BMS-986195) is a potent inhibitor of BTK with IC50 values of 0.1 nM, 0.9 nM, 1.5 nM, 5 nM for BTK, TEC, BMX, TXK, respectively. |
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S7080 |
RN486RN486 is a potent and selective BTK inhibitor with IC50 of 4 nM. |
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S9660New |
Remibrutinib (LOU064)Remibrutinib (LOU064) is a potent, highly selective covalent inhibitor of bruton tyrosine kinase (BTK) with IC50 of 1.3 nM, 2.5 nM and 18 nM for BTK, FcγR-induced IL8 and anti-IgM/IL4-induced CD69, respectively. Remibrutinib (LOU064) exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for the treatment of autoimmune diseases. |
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S9600New |
OrelabrutinibOrelabrutinib (ICP-022) is a potent, orally active and irreversible inhibitor of Bruton's tyrosine kinase (BTK). Orelabrutinib has potential antineoplastic activity. |
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S8679 |
BTK inhibitor 1 (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. |
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S7734 |
LFM-A13LFM-A13 is a specific Bruton's tyrosine kinase (BTK) inhibitor with IC50 of 2.5 μM, >100-fold selectivity over other protein kinases including JAK1, JAK2, HCK, EGFR,and IRK. |
![]() ![]() Cell-free kinase assay of IFN-gR2 phosphorylation at Y289 by constitutively active BTK with or without BTK inhibitor LFM-A13 (100 mM). WCL, whole-cell lysate; DIC, differential interference contrast microscopy.
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S7877 |
ONO-4059 analogueONO-4059 analogue (ONO-WG-307) is an analogue of ONO-4059, which is a highly potent and selective oral BTK inhibitor with IC50 of 23.9 nM. Phase 1. |
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S8294 |
Olmutinib (BI 1482694)Olmutinib (BI 1482694) is a novel third-generation epidermal growth factor receptor (EGFR) mutation-specific tyrosine kinase inhibitor (TKI). Also a potent inhibitor of Bruton's tyrosine kinase. |
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S8777 |
EvobrutinibEvobrutinib (M-2951, MSC-2364447C) is a highly selective BTK inhibitor with an IC50 of 37.9 nM. It has potential anti-neoplastic activity. |
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S8348 |
BMS-935177BMS-935177 is a potent, reversible Bruton's Tyrosine Kinase (BTK) inhibitor with an IC50 value of 2.8 nM and demonstrates good kinase selectivity. It is more potent against BTK than other kinase, including the other Tec family kinases (TEC, BMX, ITK, and TXK) over which the compound is between 5- and 67-fold selective. |
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S8381 |
BMS-986142BMS-986142 is a potent and highly selective reversible small molecule inhibitor of BTK with an IC50 of 0.5 nM. In a panel of 384 kinases, only five kinases were inhibited by BMS-986142 with less than 100-fold selectivity for BTK (TEC, ITK, BLK, TXK and BMX). |
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S8116 |
Acalabrutinib (ACP-196)Acalabrutinib (ACP-196) is a selective second-generation Bruton's tyrosine kinase (BTK) inhibitor with an IC50 of 3 nM, which prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. ACP-196 has improved target specificity over ibrutinib with 323-, 94-, 19- and 9-fold selectivity over the other TEC kinase family members (ITK, TXK, BMX, and TEC, respectively) and no activity against EGFR. |
![]() ![]() Comparison of the impairment of ADCC against primary CLL cells by different irreversible BTK inhibitors. The antibody-dependent increase in the percentages of minimal calcein retention was determined with 3-fold excess of 1708-LC3E11 effector cells over CLL target cells in seven independent experiments. (a) Asterisks above the boxes and whiskers denote the significance of enhanced cytotoxicity compared to the control without addition of antibodies and inhibitors as determined by paired t-tests. Furthermore combination treatment was compared to that with anti-CD20 antibodies as single agents. (b) The mean differences ± SEM in the cytotoxicity against CLL cells in the presence and absence of rituximab and obinutuzumab were calculated from the data shown in (a). The ADCC of rituximab and obinutuzumab was compared by paired two-tailed t-test. *p<0.05; **p<0.01; ***p<0.001.
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S8421 |
Fenebrutinib (GDC-0853)Fenebrutinib (GDC-0853) is a potent, selective, and non-covalent bruton's tyrosine kinase (BTK) inhibitor with an Ki value of 0.91 nM for Btk with >100-fold selectivity over 3 off-targets (Bmx :153-fold, Fgr: 168-fold, Src:131-fold). |
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S8791 |
Zanubrutinib (BGB-3111)Zanubrutinib (BGB-3111) is a potent, specific and irreversible BTK inhibitor that has been shown to have a lower off-target inhibitory activity on other kinases, including ITK, JAK3 and EGFR. |
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S6725 |
PCI 29732PCI 29732 is a selective and irreversible Btk inhibitor with an IC50 of 0.5 nM. |
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S7051 |
CGI1746CGI1746 is a potent and highly selective small-molecule inhibitor of the Btk with IC50 of 1.9 nM. |
![]() ![]() Cleaved IL-1β and caspase-1 from primed and nigericin-treated human primary MoMacs pretreated with DMSO (mock), ibrutinib, or CGI-1746 for 10 minutes. Pro-IL-1β and caspase-1 processing in primary MoMacs was strongly reduced by both ibrutinib and CGI1746.
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S8542 |
Btk inhibitor 2Btk inhibitor 2 is a BTK inhibitor. |
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S8166 |
tirabrutinib(ONO-4059) hydrochlorideTirabrutinib Hydrochloride (ONO-4059, GS-4059) is highly potent and selective BTK inhibitor with an IC50 of 2.2 nM. |
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S8711 |
ARQ 531ARQ 531 is an ATP-competitive tyrosine kinase inhibitor designed to target BTK with an IC50 of 0.85 nM. It also has a distinct kinase selectivity profile with strong inhibitory activity against several key oncogenic drivers from TEC, Trk and Src family kinases. |
Catalog No. | Information | Product Use Citations | Product Validations |
---|---|---|---|
S2680 |
Ibrutinib (PCI-32765)Ibrutinib (PCI-32765) is a potent and highly selective Brutons tyrosine kinase (Btk) inhibitor with IC50 of 0.5 nM in cell-free assays, modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc. Ibrutinib is applicable as a Btk ligand in the synthesis of a series of PROTACs including P13I. |
![]() ![]() Identification of Btk as a potent kinase for WIP tyrosine phosphorylation. Total protein lysates were prepared from THP-1 cells that were stably transfected with wild-type WIP-EGFP and treated with PCI-32765 at the concentration specified on the blots for 2h before pervanadate treatment for 30 min. In all cases WIP-EGFP was immunoprecipitated from cell lysates using anti-EGFP antibody and membranes subsequently blotted with the pY (4G10) antibody, EGFP antibody and β-Tubulin.
|
|
S7173 |
Spebrutinib (CC-292)Spebrutinib (CC-292, AVL-292) is a covalent, orally active, and highly selective BTK inhibitor with IC50 of <0.5 nM, displaying at least 1400-fold selectivity over the other kinases assayed. Phase 1. |
![]() ![]() Effects of AVL-292, CNX-774 and dasatinib on IgE-mediated histamine release in human basophils. Basophils (BA) obtained from three nonallergic donors (A). |
|
S7257 |
CNX-774CNX-774 is an irreversible, orally active, and highly selective BTK inhibitor with IC50 of <1 nM. |
![]() ![]() Effects of AVL-292, CNX-774 and dasatinib on IgE-mediated histamine release in human basophils. Basophils (BA) obtained from three nonallergic donors (A), three patients allergic to Der p 2, and three patients allergic to Phl p 5 (B and C) were preincubated in control medium (Co) or medium containing various concentrations of AVL-292, CNX-774, or dasatinib (0.001-1 μmol/L) at 37°C for 30 minutes. Then, cells were exposed to anti-IgE antibody E-124.2.8 (1 μg/mL; nonallergic donors) or recombinant allergens (1 μg/mL of rDer p 2 or rPhl p 5 in allergic patients) at 37°C for 30 minutes. After centrifugation, histamine concentrations were determined in cell-free supernatants and cell lysates. Histamine release is expressed as percentage of total histamine. Results show the percentage of control and represent mean SD from three independent experiments (three donors). Asterisk (*): P<0.05 by Student's t test with Bonferroni correction |
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S8832 |
Branebrutinib (BMS-986195)Branebrutinib (BMS-986195) is a potent inhibitor of BTK with IC50 values of 0.1 nM, 0.9 nM, 1.5 nM, 5 nM for BTK, TEC, BMX, TXK, respectively. |
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S7080 |
RN486RN486 is a potent and selective BTK inhibitor with IC50 of 4 nM. |
||
S9660New |
Remibrutinib (LOU064)Remibrutinib (LOU064) is a potent, highly selective covalent inhibitor of bruton tyrosine kinase (BTK) with IC50 of 1.3 nM, 2.5 nM and 18 nM for BTK, FcγR-induced IL8 and anti-IgM/IL4-induced CD69, respectively. Remibrutinib (LOU064) exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for the treatment of autoimmune diseases. |
||
S9600New |
OrelabrutinibOrelabrutinib (ICP-022) is a potent, orally active and irreversible inhibitor of Bruton's tyrosine kinase (BTK). Orelabrutinib has potential antineoplastic activity. |
||
S8679 |
BTK inhibitor 1 (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. |
||
S7734 |
LFM-A13LFM-A13 is a specific Bruton's tyrosine kinase (BTK) inhibitor with IC50 of 2.5 μM, >100-fold selectivity over other protein kinases including JAK1, JAK2, HCK, EGFR,and IRK. |
![]() ![]() Cell-free kinase assay of IFN-gR2 phosphorylation at Y289 by constitutively active BTK with or without BTK inhibitor LFM-A13 (100 mM). WCL, whole-cell lysate; DIC, differential interference contrast microscopy.
|
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S7877 |
ONO-4059 analogueONO-4059 analogue (ONO-WG-307) is an analogue of ONO-4059, which is a highly potent and selective oral BTK inhibitor with IC50 of 23.9 nM. Phase 1. |
||
S8294 |
Olmutinib (BI 1482694)Olmutinib (BI 1482694) is a novel third-generation epidermal growth factor receptor (EGFR) mutation-specific tyrosine kinase inhibitor (TKI). Also a potent inhibitor of Bruton's tyrosine kinase. |
||
S8777 |
EvobrutinibEvobrutinib (M-2951, MSC-2364447C) is a highly selective BTK inhibitor with an IC50 of 37.9 nM. It has potential anti-neoplastic activity. |
||
S8348 |
BMS-935177BMS-935177 is a potent, reversible Bruton's Tyrosine Kinase (BTK) inhibitor with an IC50 value of 2.8 nM and demonstrates good kinase selectivity. It is more potent against BTK than other kinase, including the other Tec family kinases (TEC, BMX, ITK, and TXK) over which the compound is between 5- and 67-fold selective. |
||
S8381 |
BMS-986142BMS-986142 is a potent and highly selective reversible small molecule inhibitor of BTK with an IC50 of 0.5 nM. In a panel of 384 kinases, only five kinases were inhibited by BMS-986142 with less than 100-fold selectivity for BTK (TEC, ITK, BLK, TXK and BMX). |
||
S8116 |
Acalabrutinib (ACP-196)Acalabrutinib (ACP-196) is a selective second-generation Bruton's tyrosine kinase (BTK) inhibitor with an IC50 of 3 nM, which prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. ACP-196 has improved target specificity over ibrutinib with 323-, 94-, 19- and 9-fold selectivity over the other TEC kinase family members (ITK, TXK, BMX, and TEC, respectively) and no activity against EGFR. |
![]() ![]() Comparison of the impairment of ADCC against primary CLL cells by different irreversible BTK inhibitors. The antibody-dependent increase in the percentages of minimal calcein retention was determined with 3-fold excess of 1708-LC3E11 effector cells over CLL target cells in seven independent experiments. (a) Asterisks above the boxes and whiskers denote the significance of enhanced cytotoxicity compared to the control without addition of antibodies and inhibitors as determined by paired t-tests. Furthermore combination treatment was compared to that with anti-CD20 antibodies as single agents. (b) The mean differences ± SEM in the cytotoxicity against CLL cells in the presence and absence of rituximab and obinutuzumab were calculated from the data shown in (a). The ADCC of rituximab and obinutuzumab was compared by paired two-tailed t-test. *p<0.05; **p<0.01; ***p<0.001.
|
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S8421 |
Fenebrutinib (GDC-0853)Fenebrutinib (GDC-0853) is a potent, selective, and non-covalent bruton's tyrosine kinase (BTK) inhibitor with an Ki value of 0.91 nM for Btk with >100-fold selectivity over 3 off-targets (Bmx :153-fold, Fgr: 168-fold, Src:131-fold). |
||
S8791 |
Zanubrutinib (BGB-3111)Zanubrutinib (BGB-3111) is a potent, specific and irreversible BTK inhibitor that has been shown to have a lower off-target inhibitory activity on other kinases, including ITK, JAK3 and EGFR. |
||
S6725 |
PCI 29732PCI 29732 is a selective and irreversible Btk inhibitor with an IC50 of 0.5 nM. |
||
S7051 |
CGI1746CGI1746 is a potent and highly selective small-molecule inhibitor of the Btk with IC50 of 1.9 nM. |
![]() ![]() Cleaved IL-1β and caspase-1 from primed and nigericin-treated human primary MoMacs pretreated with DMSO (mock), ibrutinib, or CGI-1746 for 10 minutes. Pro-IL-1β and caspase-1 processing in primary MoMacs was strongly reduced by both ibrutinib and CGI1746.
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S8542 |
Btk inhibitor 2Btk inhibitor 2 is a BTK inhibitor. |
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S8166 |
tirabrutinib(ONO-4059) hydrochlorideTirabrutinib Hydrochloride (ONO-4059, GS-4059) is highly potent and selective BTK inhibitor with an IC50 of 2.2 nM. |
||
S8711 |
ARQ 531ARQ 531 is an ATP-competitive tyrosine kinase inhibitor designed to target BTK with an IC50 of 0.85 nM. It also has a distinct kinase selectivity profile with strong inhibitory activity against several key oncogenic drivers from TEC, Trk and Src family kinases. |