| E1993 |
Catadegbrutinib (BGB-16673)
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Catadegbrutinib (BGB-16673) is an inhibitor of Bruton’s tyrosine kinase (Btk) and can be used in research for the treatment of autoimmune and inflammatory diseases.
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| S2680 |
Ibrutinib (PCI-32765)
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Ibrutinib 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.
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Cell Rep Med, 2025, 6(3):102027
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J Allergy Clin Immunol, 2025, 155(2):569-582
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Clin Cancer Res, 2025, 10.1158/1078-0432.CCR-25-2907
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| S8116 |
Acalabrutinib (ACP-196)
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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. This compound has improved target specificity 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.
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J Allergy Clin Immunol, 2025, 155(2):569-582
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Cancers (Basel), 2025, 17(11)1889
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bioRxiv, 2025, 2025.05.20.655210
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| S7173 |
Spebrutinib (AVL-292)
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Spebrutinib (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. It is in Phase 1.
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oparu, 2023, 10.18725/OPARU-47820
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Elife, 2021, 10e66984
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American Journal of Physiology-Cell Physiology, 2021, C902-C915
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| S8166 |
tirabrutinib(ONO-4059) hydrochloride
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Tirabrutinib Hydrochloride (ONO-4059, GS-4059) is a highly potent and selective BTK inhibitor with an IC50 of 2.2 nM.
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PLoS One, 2023, 18(8):e0290872
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Br J Pharmacol, 2022, 179(11):2754-2770
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Am J Physiol Cell Physiol, 2021, 320(5):C902-C915
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| S7051 |
CGI1746
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CGI1746 is a potent and highly selective small-molecule inhibitor of the Btk with IC50 of 1.9 nM.
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J Allergy Clin Immunol, 2025, 155(2):569-582
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Elife, 2020, 9e60470
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Am J Transl Res, 2019, 11(7):4139-4150
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| S7734 |
LFM-A13
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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.
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Br J Pharmacol, 2022, 179(11):2754-2770
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Blood Adv, 2020, 4(18):4393-4405
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Biochem Pharmacol, 2020, 172:113741
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| S7257 |
CNX-774
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CNX-774 is an irreversible, orally active, and highly selective BTK inhibitor with IC50 of <1 nM.
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Cancer Lett, 2023, 552:215981
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Br J Pharmacol, 2022, 179(11):2754-2770
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Oncol Rep, 2021, 45(5)56
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| S8777 |
Evobrutinib
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Evobrutinib is a highly selective BTK inhibitor with an IC50 of 37.9 nM. It has potential anti-neoplastic activity.
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Cancer Res Commun, 2025, 5(9):1621-1630
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Brain Pathol, 2024, e13240.
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J Leukoc Biol, 2024, qiae160
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| S8791 |
Zanubrutinib (BGB-3111)
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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.
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Acta Histochemica et Cytochemica, 2025, 93-100
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iScience, 2024, 27(10):110862
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Blood, 2023, 62-72
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