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Structure

ARQ 531, Inhibitor | ARQ531, inhibitor

ARQ 531

Purity
98.00%
Synonyms
ARQ 531; ARQ531; inhibitor
Ordering
For Research Use Only!
Purity/Purification
98.00%
Form/Format
Solid. Powder
Solubility
DMSO: 50mg/mL (104.40mM)
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C25H23ClN4O4
SMILES
O=C(C1=C(C=C(OC2=CC=CC=C2)C=C1)Cl)C3=CNC4=NC=NC(N[C@@H]5CC[C@@H](CO)OC5)=C34
CAS Number
2095393-15-8
Target & IC50
WT-BTK: ic50 0.85nM
C481S-BTK: ic50 0.39nM
In Vitro
ARQ 531 is efficacious in TMD-8 tumor xenograft model and it is also efficacious in collagen induced arthritis model. ARQ 531 causes complete tumor regression after 14 days of treatment, ARQ 531 demonstrates potent efficacy against arthritis in mouse model and it also demonstrates in vivo efficacy in a mouse collagen-induced arthritis (CIA) model[1]. In the BTK driven TMD8 xenograft mouse model, ARQ 531 demonstrates excellent anti-tumor activity with durable response.
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent

Structure

Structure
Related Product Information for ARQ531, inhibitor
ARQ 531 is a reversible non-covalent inhibitor of Bruton's Tyrosine Kinase (BTK). With IC50s of 0.85nM and 0.39nM for WT-BTK and C481S-BTK, respectively.
References
S Eathiraj, et al. Targeting Ibrutinib-Resistant BTK-C481S Mutation with ARQ 531, a Reversible Non-Covalent Inhibitor of BTK. Clinical Lymphoma Myeloma & Leukemia, 2016, 16: S47-S48.
S Eathiraj, et al. Targeting Ibrutinib-Resistant BTK-C481S Mutation with ARQ 531, a Reversible Non-Covalent Inhibitor of BTK. Clinical Lymphoma Myeloma & Leukemia, 2016, 16: S47-S48.

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Product Notes

The ARQ531 (Catalog #AAA5754532) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "ARQ 531, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.

Precautions

All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.

Disclaimer

Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.

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