ARQ 531 是一种可逆的、非共价的、具有口服活性的 BTK 抑制剂，能够作用于 WT-BTK (IC50:0.84 nM) 和 C481S-BTK (IC50:0.39 nM)。

ARQ-531 is a potent and orally active BTK inhibitor with potential antineoplastic activity, with IC50s of 0.85 nM and 0.39 nM for WT-BTK and C481S-BTK, respectively.

In vitro treatment of patient CLL cells with ARQ 531 decreases BTK-mediated functions including B-cell receptor (BCR) signaling, viability, migration, CD40 and CD86 expression, and NF-κB gene transcription.?Additionally, ARQ 531 inhibits CLL cell survival and suppresses BCR-mediated activation of C481S BTK and PLCγ2 mutants, which facilitate clinical resistance to ibrutinib[2].

In vivo, ARQ 531 was found to increase survival over ibrutinib in a murine Eμ-TCL1 engraftment model of CLL and a murine Eμ-MYC/TCL1 engraftment model resembling Richter transformation[2].

2095393-15-8

C25H23ClN4O4

478.93

DMSO:50 mg/mL (104.40 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years