Btk Inhibitor

BTK-IN-32 (compound C2) is a potent inhibitor of BTK. BTK-IN-32 activates full-length BTK and smaller multidomain BTK fragments instead of the isolated kinase domain.

Faldoritinib is a Tyrosine kinase inhibitor and antineoplastic agent.

BTK ligand-14 is a PROTAC target protein ligand that targets BTK and can be used for the synthesis of FDU73 (HY-173125).

BTK inhibitor 20 is a potent BTK inhibitor with an IC₅₀ of 8 nM.

JAK3/BTK-IN-6 (compound 14h) is a potent BTK and JAK3 dual inhibitor, with IC₅₀ values of 0.6 and 0.4 nM, respectively. JAK3/BTK-IN-6 shows good metabolic stability in human liver microsome. JAK3/BTK-IN-6 can be used for hematological and immune diseases research.

BTK-IN-25 (compound 71) is a potent inhibitor of BTK, and inhibits BTK(C481S) with an IC₅₀ value of 0.77 nM. BTK-IN-25 inhibits BTK in DOHH2 cells with an IC₅₀ value of 1 nM.

JAK3/BTK-IN-4 is a potent inhibitor of JAK3/BTK. BTK and JAK3 are two important targets for autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signalling pathway exhibits synergistic effects. JAK3/BTK-IN-4 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147953A1, compound 003)

BTK-IN-12 is a potent BTK inhibitor with IC₅₀s of 1.2 nM and 0.8 nM for wild-type BTK or mutated BTK (C481S), respectively (WO2022037649A1; compound 8).

ABBV-992 is a potent and selective BTK inhibitor. ABBV-992 can be used for the research of cancer.

Pirtobrutinib-¹³C,d₃ (LOXO-305-¹³C,d₃) is the deuterated, ¹³C-labeled Pirtobrutinib (HY-131328). Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations. Pirtobrutinib causes regression of BTK-dependent lymphoma tumors in mouse xenograft models. Pirtobrutinib is also more than 300-fold selective for BTK versus 370 other kinases tested and shows no significant inhibition of non-kinase off-targets at 1 μM.

Avitinib (Abivertinib) maleate dihydrate is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC₅₀ values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib maleate dihydrate is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib maleate dihydrate shows anticancer effects.

EGFR-IN-40 (compound 3z) is a potent BTK, EGFR, and ITK inhibitor with IC₅₀ values of 1.2 nM, 5.3 nM, and 46.1 nM, respectively.

BTK-IN-45 (Compound 6b) is a potent, reversible, and selective BTK inhibitor with an IC₅₀ of 1.14 μM. BTK-IN-45 also exhibits modest inhibition for LCK. BTK-IN-45 can be used in the research of cancers, including leukemia.

(R)-Acalabrutinib ((R)-ACP-196) is the enantiomer of Acalabrutinib (HY-17600). (R)-Acalabrutinib is an inhibitor for Bruton’s tyrosine kinase (BTK).

CTA056 is an ITK (IL-2-inducible T-cell kinase) inhibitor with an IC₅₀ of 0.1 μM. CTA056 selectively targets malignant T cells and modulates oncomirs. CTA056 induces apoptosis and is a potential therapeutic agent for the research of T-cell leukemia and lymphoma.

BTK-IN-37 (compound 8d) is a BTK inhibitor that can induce apoptosis in cancer cells. BTK-IN-37 targets BTK with K_i and IC₅₀ of 5.07 nM and 3.6 nM, respectively. BTK-IN-37 can also selectively induce enrichment of genes involved in necroptosis and pyroptosis.

BTK-IN-19 (Compound 51) is a reversible BTK inhibitor with an IC₅₀ of <0.001 μM.

BTK-IN-16 is a dual inhibitor of BTK wild type and C481S mutant of Bruton’s tyrosine kinase (BTK) with IC₅₀s of 5.1 and 4.1 μM. BTK-IN-16 can be used for the research of autoimmune diseases and chronic lymphocytic leukemia.

BTK-IN-3 (example 1) is an inhibitor of BTK. BTK-IN-3 can used to study cancer.

IQS-019 is a B cell receptor (BCR) kinase inhibitor. IQS-019 can inhibit the de-phosphorylation of constitutive and IgM-activated Syk, Lyn, and Btk. IQS-019 can inhibit cell proliferation, migration and induce apoptosis. IQS-019 exhibits antitumor activity and can be used for the research of cancer, such as B cell lymphoma.