Acalabrutinib

SKU: orb1303984

Description

Acalabrutinib (ACP-196) is an oral Bruton's tyrosine kinase (BTK) inhibitor used in research for B-cell malignancies. It blocks BCR signaling, inhibiting malignant B-cell proliferation and survival. This small molecule is applied in both in vitro and in vivo studies of diseases like chronic lymphocytic leukemia and mantle cell lymphoma.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1420477-60-6
• MW: 465.51
• Purity: 99.95% (May vary between batches)
• Formula: C₂₆H₂₃N₇O₂
• SMILES: CC#CC(=O)N1CCC[C@H]1c1nc(-c2ccc(cc2)C(=O)Nc2ccccn2)c2c(N)nccn12
• Target: BTK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (8.59 mM);DMSO:125 mg/mL (268.52 mM);Ethanol:53 mg/mL (113.85 mM)

Bioactivity

• Target IC50:
  BTK:3nM
• In Vivo:
  Acalabrutinib does not inhibit EGFR, ITK, and TEC, and does not affect the phosphorylation of EGFR at the Y1068 and Y1173 sites. It has a higher IC50 value than ibrutinib and shows almost no inhibitory activity on the kinase activities of ITK, EGFR, ERBB2, ERBB4, JAK3, BLK, FGR, FYN, HCK, LCK, LYN, SRC, and YES1. In in vitro signal detection in primary human chronic lymphocytic leukemia cells, Acalabrutinib inhibits the tyrosine phosphorylation of downstream targets ERK, IKB, and AKT.
• In Vitro:
  When administered orally to mice, ACP-196 demonstrably inhibits the expression of CD86 in CD19+ spleen cells induced by anti-IgM in a dose-dependent manner, with an ED50 of 0.34 mg/kg. This inhibition exceeded 90% of CD86 expression levels after 3 hours post-treatment.

Storage & Handling

• Storage: keep away from moisture,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, irreversible, on-target, orally, PLCγ2, lymphocytic, ERK, IKB, leukemia, Inhibitor, AKT, ACP 196, ACP196, ACP-196, Acalabrutinib, Btk, BTK, Bruton tyrosine kinase, CLL, chronic, Cys481, phosphorylation, tyrosine

Compound Identifiers

PubChem CID

71226662