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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 | Availability | Quantity |
---|---|---|---|
2 mg | $41 | In Stock | |
5 mg | $89 | In Stock | |
10 mg | $129 | In Stock | |
25 mg | $222 | In Stock | |
50 mg | $355 | In Stock | |
100 mg | $567 | In Stock | |
1 mL x 10 mM (in DMSO) | $98 | 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 | Powder: -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
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