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Acalabrutinib (ACP196)
Acalabrutinib (ACP-196) is a clinical stage, second-generation irreversible inhibitor of BTK (Bruton's tyrosine kinase). The Optically Pure Acalabrutinib (ACP-196) potently inhibits BTK activity with an IC50 of 3 nM (enzymatic assay) and EC50 of 8 nM (human whole-blood CD69 B cell activation assay) (Ref. 2). Comparing with the first-generation BTK inhibitor Ibrutinib, ACP-196 is more selective. The improved selectivity is largely attributed to the reduced intrinsic reactivity of electrophile (ACP-196’s Propiolamide vs Ibrutinib’s Acrylamide). As a result, ACP-196 was shown to have improved target specificity and in vivo coverage, thus better therapeutic indexes, over Ibrutinib. It displays minimal, or no activities against off-target kinases such as ITK, EGFR, ERBB2, ERBB4, JAK3, BLK, FGR, FYN, HCK, LCK, LYN, SRC, and YES1 (Ref 1, 2). It is currently in clinical evaluation for the treatment of CCL (Chronic Lymphocytic Leukemia).
Catalog NO: CT-ACP196
Synonym: ACP-196, ACP 196
CAS NO: 1420477-60-6
Mol. Formula: C26H23N7O2
MW: 465.5 (Refer to Certificate, batch-specific)
** A recrystallized white (with faint yellow tint) powder, clean (>99.8% by achiral HPLC), optically pure (100% by chiral HPLC) (Ref. 3), + clean 1H-NMR, + a high-precision quantitative elemental analysis. Bulk stock. Ship within 1 day.