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AZD5153, inhibitor

AZD5153

Purity
98.2%
Synonyms
AZD5153; inhibitor
Ordering
For Research Use Only!
Purity/Purification
98.2%
Form/Format
POWDER
CAS
1869912-40-2
Formula
C25H33N7O3.C11H8O3
Receptor
BD1-BRD4: 1.6uM
FL-BRD4: 5nM
Bioactivity
AZD 5153 an orally available, bivalent inhibitor of the bromodomain and extraterminal (BET) protein BRD4 (IC50 = 5 nM). It can simultaneously bind two bromodomains in BRD4, which has been shown to increase antitumor activity in multiple xenograft models of acute myeloid leukemia, multiple myeloma, and diffuse large B cell lymphoma.
Solubility
DMSO: 93mg/ml (139.3 mM)
Water: <1mg/ml
Ethanol: 26mg/ml (38.9 mM)
Cell Assay
Apoptosis was analyzed by flow cytometry using Cell Event Caspase 3/7 Green detection reagent. MV-4-11, MM.1S, and K562 cells were pretreated with AZD5153 or I-BET762 for 48 hours in culture media. Cells were collected and stained with 5 μmol/Lfinal concentration of Cell Event for 30 minutes at 37°C. Flow cytometry was done on a BD Fortessa using the Blue laser and FITC filter set. (Only for Reference)
Preparation and Storage
For 3 years at -20 degree C powder
For 2 years -80 degree C in solvent.
References
1. Rhyasen, G.W.,Hattersley, M.M.,Yao, Y., et al. AZD5153: A novel bivalent BET bromodomain inhibitor highly active against hematologic malignancies. Mol. Cancer Ther. 2016, 15 (11), 2563-2574.

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Product Notes

The AZD5153 (Catalog #AAA579634) 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 "AZD5153, 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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