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Acalabrutinib (ACP196)
Acalabrutinib (ACP-196) is a second-generation, potent and selective 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).
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)
** in vivo Quality Material. 99.8% Pure by Achiral and Chiral HPLCs (attached). Hydrate, verified by a spot-on Elemental Analysis. Bulk stock (Discounted price for 0.2, 0.5, 1G, …). Same Day Shipping.