ARQ 531

SKU: orb1308638

Description

ARQ 531

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 2095393-15-8
• MW: 478.93
• Purity: 99.63%
• Formula: C₂₅H₂₃ClN₄O₄
• SMILES: OC[C@@H]1CC[C@H](CO1)Nc1ncnc2[nH]cc(C(=O)c3ccc(Oc4ccccc4)cc3Cl)c12
• Target: BTK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.18 mM);DMSO:50 mg/mL (104.4 mM)

Bioactivity

• Target IC50:
  BTK (C481S):0.39 nM|BTK (WT):0.85 nM
• In Vivo:
  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.
• In Vitro:
  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.

Storage & Handling

• Storage: store at low temperature | 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

ARQ 531, ARQ531, ARQ-531, Btk, C481S-BTK, Bruton tyrosine kinase, inhibit, MK1026, MK-1026, MK 1026, Inhibitor, WT-BTK

Compound Identifiers

PubChem CID

129045720