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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 Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $41 | In Stock | In Stock | |
| 5 mg | $89 | In Stock | In Stock | |
| 10 mg | $129 | In Stock | In Stock | |
| 25 mg | $222 | In Stock | In Stock | |
| 50 mg | $355 | In Stock | In Stock | |
| 100 mg | $567 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $98 | In Stock | In Stock |
| 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]. |
| Molecular Weight | 478.93 |
| Formula | C25H23ClN4O4 |
| Cas No. | 2095393-15-8 |
| Smiles | OC[C@@H]1CC[C@H](CO1)Nc1ncnc2[nH]cc(C(=O)c3ccc(Oc4ccccc4)cc3Cl)c12 |
| Relative Density. | no data available |
| 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. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 50 mg/mL (104.4 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.18 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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