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ARQ 531

🥰Excellent
Catalog No. T14323Cas No. 2095393-15-8

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.

ARQ 531

ARQ 531

🥰Excellent
Purity: 99.59%
Catalog No. T14323Cas No. 2095393-15-8
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.
Pack SizePriceAvailabilityQuantity
2 mg$41In Stock
5 mg$89In Stock
10 mg$129In Stock
25 mg$222In Stock
50 mg$355In Stock
100 mg$567In Stock
1 mL x 10 mM (in DMSO)$98In Stock
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Purity:99.59%
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Product Introduction

Bioactivity
Description
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.
Targets&IC50
BTK (C481S):0.39 nM, BTK (WT):0.85 nM
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[2].
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[2].
Chemical Properties
Molecular Weight478.93
FormulaC25H23ClN4O4
Cas No.2095393-15-8
SmilesOC[C@@H]1CC[C@H](CO1)Nc1ncnc2[nH]cc(C(=O)c3ccc(Oc4ccccc4)cc3Cl)c12
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 50 mg/mL (104.40 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0880 mL10.4399 mL20.8799 mL104.3994 mL
5 mM0.4176 mL2.0880 mL4.1760 mL20.8799 mL
10 mM0.2088 mL1.0440 mL2.0880 mL10.4399 mL
20 mM0.1044 mL0.5220 mL1.0440 mL5.2200 mL
50 mM0.0418 mL0.2088 mL0.4176 mL2.0880 mL
100 mM0.0209 mL0.1044 mL0.2088 mL1.0440 mL

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