MedChemExpress - Model AZD5153 6-Hydroxy-2-naphthoic acid -1869912-40-2
AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor; disrupts BRD4 with an IC50 of 1.7 nM.MCE products for research use only. We do not sell to patients.
AZD5153 6-Hydroxy-2-naphthoic acid
MCE China：AZD5153 6-Hydroxy-2-naphthoic acid
Brand：MedChemExpress (MCE)
Cat. No.HY-100653A
CAS：1869912-40-2
Purity：99.80%
Storage：4°C, sealed storage, away from moisture *In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
Shipping：Room temperature in continental US; may vary elsewhere.
Description：AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor; disrupts BRD4 with an IC50 of 1.7 nM.
In Vitro：AZD5153 demonstrates a remarkable enhancement in potency for the displacement of full-length BRD4 relative to BD1, with IC50 values of 5.0 nM and 1.6 μM, respectively. AZD5153 potently disrupts BRD4 foci in U2OS cells with an IC50 value of 1.7 nM. AZD5153 efficiently down-regulates MYC protein levels across the cell line panel irrespective of their sensitivity to AZD5153[1].
In Vivo：Administration of AZD5153 leads to tumor stasis or regression in multiple xenograft models of acute myeloid leukemia, multiple myeloma, and diffuse large B-cell lymphoma. AZD5153 treatment markedly impacts transcriptional programs of MYC, E2F, and mTOR[1].
Animal Administration：Mice: Mice are treated with either vehicle (0.5% hydroxymethylcellulose, 0.1% Tween80) or AZD5153 by oral gavage mini-pump infusion. For continuous administration of AZD5153, compound is solubilized in 20% v/v DMSO/60% v/v HP-B-CD in water, loaded into a mini pump and implanted subcutaneously in mice. Tumor fragments collected are snap frozen or fixed in 10% buffered formalin. Blood samples are collected from the same mice and stabilized in EDTA. Plasma concentrations are determined by liquid chromatography/tandem mass spectrometry method[1].
IC50 & Target：IC50: 1.7 nM (BRD4)[1] In Vitro AZD5153 demonstrates a remarkable enhancement in potency for the displacement of full-length BRD4 relative to BD1, with IC50 values of 5.0 nM and 1.6 μM, respectively. AZD5153 potently disrupts BRD4 foci in U2OS cells with an IC50 value of 1.7 nM. AZD5153 efficiently down-regulates MYC protein levels across the cell line panel irrespective of their sensitivity to AZD5153[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> AZD5153 6-Hydroxy-2-naphthoic acid Related Antibodies
Hot selling product：Nobiletin | Favipiravir | DSPE-PEG2000-Maleimide | Ivosidenib | C16-Ceramide | Siltuximab | 9-cis-Retinoic acid | VER-155008 | D18 | GYY4146
Trending products：Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides
References：
[1]. Rhyasen GW, et al. AZD5153: A Novel Bivalent BET Bromodomain Inhibitor Highly Active against Hematologic Malignancies. Mol Cancer Ther. 2016 Nov;15(11):2563-2574. [Content Brief]
Brand introduction:
• MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
• More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
• The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects；
• Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
• It has a professional experimental center and strict quality control and verification system；
• Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
• The biological activity of the products has been verified by the experiments of customers in various countries；
• A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
• Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
• It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。