Acalabrutinib - ACP-196

Based on 485 reference(s) in Google Scholar 8 10 485

Axon 4141

CAS [1420477-60-6]

MF C26H23N7O2
MW 465.51

  • Purity: 99%
  • Optical purity: Optically pure
  • Soluble in DMSO
Recently added

Acalabrutinib

Description

Acalabrutinib is a second-generation irreversible inhibitor of BTK (Bruton's tyrosine kinase). The optically pure Acalabrutinib 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). Comparing with the first-generation BTK inhibitor Ibrutinib, Acalabrutinib is more selective. The improved selectivity is largely attributed to the reduced intrinsic reactivity of electrophile (Acalabrutinib’s Propiolamide vs Ibrutinib’s acrylamide). As a result, Acalabrutinib 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.

Keywords: Acalabrutinib | Supplier | BTK inhibitor | ACP-196 | ACP196 | ACP 196 | CT-ACP196 | CAS [1420477-60-6] | B-Cell transformation | BTK | Inhibitor | Enzymes

Orally active, irreversible, and highly selective second-generation BTK inhibitor

Chemical name

(S)-4-(8-amino-3-(1-but-2-ynoylpyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide

Source information

Sold in collaboration with Chemietek

Parent CAS No.

[1420477-60-6]

The purity of Axon Ligands™ is confirmed by HPLC-MS, 1H-NMR and/or microanalysis. Analytical data are available upon request.

Caution: Axon Ligands™ are not fully tested. They are for research purposes only! Not for human consumption!

Please wait...