cys481

Acalabrutinib (ACP-196), also known as ACP-196, is an orally available inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity. Upon administration, ACP-196 inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and BTK-mediated activation of downstream survival pathways. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. BTK, a member of the src-related BTK/Tec family of cytoplasmic tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role in B lymphocyte development, activation, signaling, proliferation and survival.

BTK inhibitor 17 is a potent irreversible Bruton's tyrosine kinase (BTK) inhibitor with an IC50 value of 2.1 nM, suitable for use in rheumatoid arthritis studies.

Acalabrutinib maleate is an orally active, irreversible, highly selective second-generation BTK inhibitor. It forms a covalent bond with the Cys481 residue in the ATP-binding pocket of BTK. This compound demonstrates potent targeting effects and activity in a murine model of chronic lymphocytic leukemia (CLL) and is used in CLL research. Acalabrutinib maleate acts as a click chemistry reagent, containing an alkyne group that can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules.

Poseltinib is an orally active, selective, and irreversible inhibitor of Bruton's tyrosine kinase (BTK), with an IC50 value of 1.95 nM. Poseltinib demonstrates 0.3-, 2.3-, and 2.4-fold higher selectivity for BTK over BMX, TEC, and TXK, respectively. Poseltinib covalently binds to cysteine 481 in BTK’s active site, thereby inhibiting BCR-, FcR-, and TLR-mediated signaling pathways.

GNE-431 is a potent, selective and noncovalent Btk inhibitor with IC50 of 3.2 nM. GNE-431 showed excellent potency against the C481R, T474I, and T474M mutants. GNE-431 may provide a treatment option to patients, especially those who have acquired resistance to ibrutinib by mutation of Cys481 or Thr474.

Acalabrutinib-D4 is a deuterated compound of Acalabrutinib. Acalabrutinib (T3626) has a CAS number of 1420477-60-6. Acalabrutinib, also known as ACP-196, is an orally available inhibitor of Bruton’s tyrosine kinase (BTK) with potential antineoplastic activity. Upon administration, ACP-196 inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and BTK-mediated activation of downstream survival pathways. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. BTK, a member of the src-related BTK/Tec family of cytoplasmic tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role in B lymphocyte development, activation, signaling, proliferation and survival.