BTK

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BTK Signaling Pathway Map

BTK Signaling Pathways

BTK Products

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  • BTK Inhibitors (25)
  • New BTK Products
Catalog No. Product Name Information Product Use Citations Product Validations
E0041New Tolebrutinib (SAR442168) Tolebrutinib (SAR442168, PRN2246, BTKi'168, BTKi('168)) is an oral, CNS-penetrant, irreversible inhibitor of Bruton's tyrosine kinase (BTK) with IC50s of 0.4 nM and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively.
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.
Transl Oncol, 2022, 15(1):101305
Cancer Cell, 2021, 39(3):380-393.e8
Immunity, 2021, 54(10):2273-2287.e6
S6725 PCI 29732 PCI 29732 is a selective and irreversible Btk inhibitor with an IC50 of 0.5 nM.
S6966New MT-802 MT-802 is a potent PROTAC that induces Bruton's tyrosine kinase (BTK) knockdown. MT-802 recruits BTK to the cereblon E3 ubiquitin ligase complex to trigger BTK ubiquitination and degradation via the proteasome. MT-802 has potential for treatment of C481S mutant chronic lymphocytic leukemia (CLL).
S7051 CGI1746 CGI1746 is a potent and highly selective small-molecule inhibitor of the Btk with IC50 of 1.9 nM.
Elife, 2020, 9e60470
Elife, 2020, 9e60470
Am J Transl Res, 2019, 11(7):4139-4150
S7080 RN486 RN486 is a potent and selective BTK inhibitor with IC50 of 4 nM.
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.
Elife, 2021, 10e66984
Am J Physiol Cell Physiol, 2021, 320(5):C902-C915
Elife, 2020, 9e60470
S7257 CNX-774 CNX-774 is an irreversible, orally active, and highly selective BTK inhibitor with IC50 of <1 nM.
Oncol Rep, 2021, 45(5)56
Allergy, 2017, 10.1111/all.13166
Biol Chem, 2017, 398(12):1335-1346
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.
Biochem Pharmacol, 2020, 172:113741
Blood Adv, 2020, 4(18):4393-4405
Nat Cell Biol, 2019, 21(6):778-790
S7877 ONO-4059 analogue ONO-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.
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.
Haematologica, 2021, 10.3324/haematol.2021.278743
Cell Death Dis, 2021, 12(11):1061
Front Immunol, 2021, 12:737988
S8166 tirabrutinib(ONO-4059) hydrochloride Tirabrutinib Hydrochloride (ONO-4059, GS-4059) is highly potent and selective BTK inhibitor with an IC50 of 2.2 nM.
Am J Physiol Cell Physiol, 2021, 320(5):C902-C915
J Clin Invest, 2020, 2;138448
[email protected], 2020, 51
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.
Cancer Cell, 2019, 10.1016/j.ccell.2019.09.001
Sci Rep, 2019,
J Thorac Oncol, 2019, 14(9):1556-1566
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.
Am J Physiol Cell Physiol, 2021, 320(5):C902-C915
[email protected], 2020, 51
[email protected], 2020, None
S8381 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).
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).
Am J Physiol Cell Physiol, 2021, 320(5):C902-C915
Blood Adv, 2020, 4(18):4393-4405
[email protected], 2020, 51
S8542 Btk inhibitor 2 Btk inhibitor 2 is a BTK inhibitor.
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.
S8711 Nemtabrutinib (ARQ 531) Nemtabrutinib (ARQ 531, MK-1026) 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.
Blood, 2021, blood.2021011787
S8777 Evobrutinib (M-2951) Evobrutinib (M-2951, MSC-2364447C) is a highly selective BTK inhibitor with an IC50 of 37.9 nM. It has potential anti-neoplastic activity.
Blood, 2021, blood.2021011787
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.
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.
Am J Physiol Cell Physiol, 2021, 320(5):C902-C915
[email protected], 2020, 51
[email protected], 2020, None
S9600 Orelabrutinib (ICP-022) Orelabrutinib (ICP-022) is a potent, orally active and irreversible inhibitor of Bruton's tyrosine kinase (BTK). Orelabrutinib has potential antineoplastic activity.
S9660 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.
S9825New Pirtobrutinib (LOXO-305)

Pirtobrutinib (LOXO-305, LY 3527727, RXC-005) is a highly selective, non-covalent, next generation BTK inhibitor with an IC50 of 5.69 nM in WT BTK HEK cells. Pirtobrutinib shows more than 300-fold selective for BTK over 98% of 370 other kinases.

E0041New Tolebrutinib (SAR442168) Tolebrutinib (SAR442168, PRN2246, BTKi'168, BTKi('168)) is an oral, CNS-penetrant, irreversible inhibitor of Bruton's tyrosine kinase (BTK) with IC50s of 0.4 nM and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively.
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.
Transl Oncol, 2022, 15(1):101305
Cancer Cell, 2021, 39(3):380-393.e8
Immunity, 2021, 54(10):2273-2287.e6
S6725 PCI 29732 PCI 29732 is a selective and irreversible Btk inhibitor with an IC50 of 0.5 nM.
S6966New MT-802 MT-802 is a potent PROTAC that induces Bruton's tyrosine kinase (BTK) knockdown. MT-802 recruits BTK to the cereblon E3 ubiquitin ligase complex to trigger BTK ubiquitination and degradation via the proteasome. MT-802 has potential for treatment of C481S mutant chronic lymphocytic leukemia (CLL).
S7051 CGI1746 CGI1746 is a potent and highly selective small-molecule inhibitor of the Btk with IC50 of 1.9 nM.
Elife, 2020, 9e60470
Elife, 2020, 9e60470
Am J Transl Res, 2019, 11(7):4139-4150
S7080 RN486 RN486 is a potent and selective BTK inhibitor with IC50 of 4 nM.
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.
Elife, 2021, 10e66984
Am J Physiol Cell Physiol, 2021, 320(5):C902-C915
Elife, 2020, 9e60470
S7257 CNX-774 CNX-774 is an irreversible, orally active, and highly selective BTK inhibitor with IC50 of <1 nM.
Oncol Rep, 2021, 45(5)56
Allergy, 2017, 10.1111/all.13166
Biol Chem, 2017, 398(12):1335-1346
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.
Biochem Pharmacol, 2020, 172:113741
Blood Adv, 2020, 4(18):4393-4405
Nat Cell Biol, 2019, 21(6):778-790
S7877 ONO-4059 analogue ONO-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.
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.
Haematologica, 2021, 10.3324/haematol.2021.278743
Cell Death Dis, 2021, 12(11):1061
Front Immunol, 2021, 12:737988
S8166 tirabrutinib(ONO-4059) hydrochloride Tirabrutinib Hydrochloride (ONO-4059, GS-4059) is highly potent and selective BTK inhibitor with an IC50 of 2.2 nM.
Am J Physiol Cell Physiol, 2021, 320(5):C902-C915
J Clin Invest, 2020, 2;138448
[email protected], 2020, 51
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.
Cancer Cell, 2019, 10.1016/j.ccell.2019.09.001
Sci Rep, 2019,
J Thorac Oncol, 2019, 14(9):1556-1566
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.
Am J Physiol Cell Physiol, 2021, 320(5):C902-C915
[email protected], 2020, 51
[email protected], 2020, None
S8381 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).
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).
Am J Physiol Cell Physiol, 2021, 320(5):C902-C915
Blood Adv, 2020, 4(18):4393-4405
[email protected], 2020, 51
S8542 Btk inhibitor 2 Btk inhibitor 2 is a BTK inhibitor.
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.
S8711 Nemtabrutinib (ARQ 531) Nemtabrutinib (ARQ 531, MK-1026) 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.
Blood, 2021, blood.2021011787
S8777 Evobrutinib (M-2951) Evobrutinib (M-2951, MSC-2364447C) is a highly selective BTK inhibitor with an IC50 of 37.9 nM. It has potential anti-neoplastic activity.
Blood, 2021, blood.2021011787
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.
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.
Am J Physiol Cell Physiol, 2021, 320(5):C902-C915
[email protected], 2020, 51
[email protected], 2020, None
S9600 Orelabrutinib (ICP-022) Orelabrutinib (ICP-022) is a potent, orally active and irreversible inhibitor of Bruton's tyrosine kinase (BTK). Orelabrutinib has potential antineoplastic activity.
S9660 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.
S9825New Pirtobrutinib (LOXO-305)

Pirtobrutinib (LOXO-305, LY 3527727, RXC-005) is a highly selective, non-covalent, next generation BTK inhibitor with an IC50 of 5.69 nM in WT BTK HEK cells. Pirtobrutinib shows more than 300-fold selective for BTK over 98% of 370 other kinases.

E0041New Tolebrutinib (SAR442168) Tolebrutinib (SAR442168, PRN2246, BTKi'168, BTKi('168)) is an oral, CNS-penetrant, irreversible inhibitor of Bruton's tyrosine kinase (BTK) with IC50s of 0.4 nM and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively.
S6966New MT-802 MT-802 is a potent PROTAC that induces Bruton's tyrosine kinase (BTK) knockdown. MT-802 recruits BTK to the cereblon E3 ubiquitin ligase complex to trigger BTK ubiquitination and degradation via the proteasome. MT-802 has potential for treatment of C481S mutant chronic lymphocytic leukemia (CLL).
S9825New Pirtobrutinib (LOXO-305)

Pirtobrutinib (LOXO-305, LY 3527727, RXC-005) is a highly selective, non-covalent, next generation BTK inhibitor with an IC50 of 5.69 nM in WT BTK HEK cells. Pirtobrutinib shows more than 300-fold selective for BTK over 98% of 370 other kinases.