BTK

Signaling Pathway Map

Research Area

Inhibitory Selectivity

BTK Products

New BTK Products
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.

S7173

Spebrutinib (CC-292, AVL-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.

S7257

CNX-774

CNX-774 is an irreversible, orally active, and highly selective BTK inhibitor with IC50 of <1 nM.

S8832New

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.

S7080

RN486

RN486 is a potent and selective BTK inhibitor with IC50 of 4 nM.

S8791New

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.

S8421New

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).

S8381New

BMS-986142

BMS-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).

S8777New

Evobrutinib

Evobrutinib is a highly selective BTK inhibitor with an IC50 of 37.9 nM. It has potential anti-neoplastic activity.

S8679New

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-A13

LFM-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.

S7877

ONO-4059 analogue

ONO-4059 analogue 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 (HM61713, BI 1482694)

Olmutinib 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.

S8348

BMS-935177

BMS-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.

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.

S7051

CGI1746

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

S8542

Btk inhibitor 2

Btk inhibitor 2 is a BTK inhibitor.

S8166

tirabrutinib(GS-4059/ONO-4059) hydrochloride

ONO-4059 (GS-4059) is highly potent and selective BTK inhibitor with an IC50 of 2.2 nM.

S8711

ARQ 531

ARQ 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.

S7173

Spebrutinib (CC-292, AVL-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.

S7257

CNX-774

CNX-774 is an irreversible, orally active, and highly selective BTK inhibitor with IC50 of <1 nM.

S8832New

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.

S7080

RN486

RN486 is a potent and selective BTK inhibitor with IC50 of 4 nM.

S8791New

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.

S8421New

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).

S8381New

BMS-986142

BMS-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).

S8777New

Evobrutinib

Evobrutinib is a highly selective BTK inhibitor with an IC50 of 37.9 nM. It has potential anti-neoplastic activity.

S8679New

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-A13

LFM-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.

S7877

ONO-4059 analogue

ONO-4059 analogue 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 (HM61713, BI 1482694)

Olmutinib 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.

S8348

BMS-935177

BMS-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.

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.

S7051

CGI1746

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

S8542

Btk inhibitor 2

Btk inhibitor 2 is a BTK inhibitor.

S8166

tirabrutinib(GS-4059/ONO-4059) hydrochloride

ONO-4059 (GS-4059) is highly potent and selective BTK inhibitor with an IC50 of 2.2 nM.

S8711

ARQ 531

ARQ 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.