Acalabrutinib (formerly known as ACP196; ACP-196; trade name: Calquence) is a selective second-generation Bruton’s tyrosine kinase (BTK) inhibitor with anticancer activity.

BMX-IN-1 is a novel, potent, selective and covalent / irreversible BMX (bone marrow tyrosine kinase on chromosome X) inhibitor with the potential for treating prostate cancer.

PCI-33380 is a novel and irreversible Bruton’s Tyrosine Kinase (BTK) inhibitor that was designed based on the ibrutinib scaffold in combination with a fluorescent probe, and has been used in both cellular and in vivo studies that demonstrated the connection between the inhibitor binding event and phenotypic readouts of cellular responses due to the inhibition […]

N-piperidine Ibrutinib HCl, the hydrochloride salt of N-piperidine Ibrutinib, is an intermediate used in the synthesis of BTK-targeted PROTACs such as SJF620 (DC50 of 7.9 nM for degrading BTK).

QL-47 (also known as QL-XII-47) is a novel, potent, selective and irreversible BTK kinase inhibitor with IC50 of 7 nM.

BMS-935177 is a potent, selective, reversible, and 2nd generation inhibitor of Bruton’s Tyrosine Kinase (BTK) with an IC50 of 3 nM.

MT-802 is a novel and potent PROTAC-mediated degrader which binds fewer off-target kinases than ibrutinib does, thereby inducing BTK knockdown, and recruiting BTK to the cereblon E3 ubiquitin ligase complex to trigger BTK ubiquitination and degradation via the proteasome.

Fenebrutinib (formerly RG-7845; GDC-0853) is a novel, potent, selective, orally bioavailable, and noncovalent (reversible) bruton’s tyrosine kinase (BTK) inhibitor (Ki = 0.91 nM) with anticancer and anti-inflammatory activity.

Pirtobrutinib (formerly LOXO-305; LY-3527727; Jaypirca) is a novel, highly selective and non-covalent next generation BTK (Bruton’s tyrosine kinase) inhibitor which inhibits diverse BTK C481 substitution mutations.

GDC-0834 Racemate is a novel, potent and selective BTK inhibitor with an in vitro IC50 of 5.9 and 6.4 nM in biochemical and cellular assays, respectively, and in vivo IC50 of 1.1 and 5.6 μM in mouse and rat, respectively.