ARQ 531

Catalog No.S8711

ARQ 531 Chemical Structure

Molecular Weight(MW): 478.93

ARQ 531 is an ATP-competitive tyrosine kinase inhibitor designed to target BTK with an IC50 of 0.85 nM. It also has a distinct kinase selectivity profile with strong inhibitory activity against several key oncogenic drivers from TEC, Trk and Src family kinases.

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Biological Activity

Description ARQ 531 is an ATP-competitive tyrosine kinase inhibitor designed to target BTK with an IC50 of 0.85 nM. It also has a distinct kinase selectivity profile with strong inhibitory activity against several key oncogenic drivers from TEC, Trk and Src family kinases.
Targets
BTK [1]
(Cell-free assay)
BRK [1]
(Cell-dree)
BRK [1]
(Cell-free assay)
LCK [1]
(Cell-free)
LCK [1]
(Cell-free assay)
0.85 nM 2.45 nM 2.45 nM 3.86 nM 3.86 nM
In vitro

ARQ 531 potently inhibited BTK (IC50 = 0.85 nM), the binding potency was accompanied by long residence time (51 min). ARQ 531 selectively inhibits BCR signaling dependent PI3K/AKT/mTOR, Ras/Raf/Erk and Rap-GTPase-Cofilin pathways in TMD8 cells. It potently inhibits proliferation of hematological malignant cell lines both sensitive and resistant to ibrutinib addicted to BCR signaling[1]. Unlike ibrutinib, ARQ 531 suppressed both the upstream activating signals (via inhibition of a select member of Src kinase family) and the downstream signaling pathways (via pAKT and pERK kinases). In GCB-DLBCL cell lines (SUDHL-4 and DOHH-2), ARQ 531 potently suppressed expression of anti-apoptotic c-Myc and BCL6 oncoproteins in a dose dependent fashion, and concomitantly induced apoptotic cleavage of PARP protein[2].

In vivo

ARQ 531 has potent anti-tumor activity was observed in both ABC-DLBCL and GCB-DLBCL mouse xenograft models[1]. ARQ 531 crosses the blood, brain-barrier[2]. In a single oral dose study of 10mg/kg in monkeys, the bioavailability of ARQ 531 is 72.4% with a Cmax of 9 μM and a half-life greater than 24 hours[3].

Protocol

Cell Research:

[3]

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  • Cell lines: CLL cells
  • Concentrations: 0.1 μM, 1.0 μM, or 10.0 μM
  • Incubation Time: 72 h
  • Method:

    --


    (Only for Reference)
Animal Research:

[3]

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  • Animal Models: B6 mice engrafted with 1E7 CD5+/CD19+ TCL1 lymphocytes via tail vein injection
  • Formulation: --
  • Dosages: 50 or 75 mg/kg
  • Administration: by oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 95 mg/mL (198.35 mM)
Ethanol 7 mg/mL (14.61 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 478.93
Formula

C25H23ClN4O4

CAS No. 2095393-15-8
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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BTK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID