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BTK Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
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 this compound is between 5- and 67-fold selective.
iScience, 2021, 24(9):102931
Am J Physiol Cell Physiol, 2021, 320(5):C902-C915
ScholarsArchive@OSU, 2020, 51
S8421 Fenebrutinib (GDC-0853) Fenebrutinib (GDC-0853) is a potent, selective, and non-covalent bruton's tyrosine kinase (BTK) inhibitor with a Ki value of 0.91 nM for Btk. This compound exhibits >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
ScholarsArchive@OSU, 2020, 51
S8791 Zanubrutinib (BGB-3111) Zanubrutinib 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.
iScience, 2024, 27(10):110862
J Clin Invest, 2023, 133(2)e163498
UNIVERSITY OF PADUA, 2023,
S9825 Pirtobrutinib (LOXO-305)

LOXO-305 (Pirtobrutinib, 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. This compound shows more than 300-fold selective for BTK over 98% of 370 other kinases.
J Clin Invest, 2024, 134(23)e173770
J Clin Invest, 2023, 133(3)e165694
E2838 M7583 M7583 is a potent, orally active, ATP-competitive, and highly selective irreversible BTK inhibitor with IC50 and Ki of 1.5 nM and 11.9 nM, respectively.
Cancer Res Commun, 2025, 5(9):1621-1630
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 this compound with less than 100-fold selectivity for BTK (TEC, ITK, BLK, TXK and BMX).
BMC Oral Health, 2023, 23(1):265
S8711 Nemtabrutinib (ARQ 531) An ATP-competitive tyrosine kinase inhibitor, Nemtabrutinib (ARQ 531, MK-1026) is 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
S7080 RN486 RN486 is a potent and selective BTK inhibitor with IC50 of 4 nM.
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.
E1381 NX-2127 NX-2127 is a unique, potent inhibitor of BTK that prevents its functions by catalyzing the ubiquitylation and proteasomal degradation of BTK rather than via direct binding. This compound stimulates T cell activation and increases IL-2 production in primary human T Cells.
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.
E1660 NX-5948 NX-5948(BTK-IN-24) is a novel oral small molecule that induces BTK degradation via cereblon E3 ubiquitin ligase recruitment. It mediates potent anti-inflammatory activity and can cross the blood-brain barrier in animal models.
E2843 Poseltinib Poseltinib (HM71224, LY3337641) shows a highly selective inhibition for Bruton’s tyrosine kinase (BTK) with IC50 of 1.95 nM, in which the selectivity toward other BMX, TEC and TXK are 0.3, 2.3 and 2.4 fold, respectively. 
E1848 BGB-8035 BGB-8035 is an orally active, highly selective inhibitor of Bruton's tyrosine kinase (BTK) with IC50 values of 1.1 nM for BTK, respectively. This compound exhibits antitumor and anti-arthritis activity and displays potential for its use in research of B-cell malignancies and autoimmune diseases.
E1582 Edralbrutinib Edralbrutinib (TG-1701) is an irreversible, highly specific, and potent inhibitor of Bruton's tyrosine kinase (BTK). TG-1701 shows similar efficacy but greater selectivity compared to the first-in-class BTK inhibitor ibrutinib, with a Kd value of 3 nmol/L, in both in vitro and in vivo models of B-cell non-Hodgkin lymphoma (B-NHL).
E1611 Atuzabrutinib Atuzabrutinib (SAR 444727, PRN473) is a reversible, selective inhibitor of Bruton's tyrosine kinase (Btk). It can effectively prevent neutrophil recruitment via inhibition of macrophage antigen‐1 signalling.
S6966 MT-802 MT-802 is a potent PROTAC that induces Bruton's tyrosine kinase (BTK) knockdown. This compound recruits BTK to the cereblon E3 ubiquitin ligase complex to trigger BTK ubiquitination and degradation via the proteasome. It has potential for treatment of C481S mutant chronic lymphocytic leukemia (CLL).
E1355 JNJ-64264681 JNJ-64264681 is an orally active, irreversible covalent inhibitor of Bruton's tyrosine kinase (BTK) with potent whole blood activity and exceptional kinome selectivity. It exhibits potential efficacy in treatment for B-cell malignancies and autoimmune disorders.
S9717 Vecabrutinib Vecabrutinib (SNS-062) is a potent, noncovalent BTK and ITK inhibitor, with Kd values of 0.3 nM and 2.2 nM, respectively. Vecabrutinib shows an IC50 of 24 nM for ITK.
E4643 BIIB129 BIIB129, is a unique brain-penetrant covalent inhibitor of Bruton’s tyrosine kinase (BTK), with high kinome selectivity. It exhibits efficacy in targeting B-cell proliferation in the central nervous system (CNS), making it a promising immunomodulatory therapy for multiple sclerosis (MS).
S9660 Remibrutinib Remibrutinib 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. This compound exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for the treatment of autoimmune diseases.
S8571 BTK IN-1 BTK IN-1(SNS062 analog) is a potent Bruton's tyrosine kinase (BTK) inhibitor, with an IC50 of <100 nM.
E0041 Tolebrutinib Tolebrutinib 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.
S6725 PCI 29732 PCI 29732 is a selective and irreversible Btk inhibitor with an IC50 of 0.5 nM.
E2201 N-piperidine Ibrutinib hydrochloride N-piperidine Ibrutinib hydrochloride, a reversible Ibrutinib derivative, is a potent BTK inhibitor with IC50s of 51.0 and 30.7 nM for WT BTK and C481S BTK, respectively.
S9600 Orelabrutinib Orelabrutinib is a potent, orally active and irreversible inhibitor of Bruton's tyrosine kinase (BTK). This compound has potential antineoplastic activity.
E1625 Elsubrutinib Elsubrutinib(ABBV-105) is a covalent, irreversible, potent, and highly selective inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 0.18 μM for BTK catalytic domain. It specifically inhibits BTK dependent cellular functions, including both BCR and FcγR mediated signaling. It also exhibits significant efficacy in pre-clinical mechanistic models of antibody production, as well as in models of rheumatoid arthritis and lupus.
S8542 Btk inhibitor 2 Btk inhibitor 2 is a BTK inhibitor.
S9944 PRN1008 PRN1008 (Rilzabrutinib) is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 1.3 nM.
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.
iScience, 2024, 27(10):110862
Br J Pharmacol, 2022, 179(11):2754-2770
Ther Adv Med Oncol, 2022, 14:17588359221079125
S8741 Avitinib (Abivertinib) Avitinib (Abivertinib) is a pyrrolopyrimidine-based irreversible EGFR inhibitor that is mutation-selective with IC50 value of 0.18 nM against EGFR L858R/T790M double mutations, nearly 43-fold greater potency over wild-type EGFR (IC50 value, 7.68 nM). It has comparable anti-tumor activity and tolerated toxicity.
iScience, 2024, 27(10):110862
Microsyst Nanoeng, 2023, 9:57
, 2022, 10.21203/rs.3.rs-2146794/v1
E4597 Avitinib maleate Avitinib maleate(Abivertinib maleate, AC0010 maleate, AC0010MA) is a third-generation, irreversible, and orally active selective inhibitor of EGFR. It displays IC50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M, and wild-type EGFR. This compound also acts as an inhibitor of BTK that induces apoptosis of BTK in mantle cell lymphoma.