| Name | AZD5153 6-Hydroxy-2-naphthoic acid |
| Description | AZD5153 6-Hydroxy-2-naphthoic acid (AZD5153) is a potent triazolopyridazine-based Bromodomain (BRD4) and Extraterminal (BET) inhibitor utilized in cancer treatments. |
| Cell Research | Apoptosis was analyzed by flow cytometry using CellEvent 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/L final concentration of CellEvent 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) |
| In vitro | AZD5153 treatment markedly affects transcriptional programs of MYC, E2F, and mTOR. Of note, mTOR pathway modulation is associated with cell line sensitivity to AZD5153. AZD5153 potently disrupts BRD4 foci in U2OS cells with an IC50 value of 1.7 nmol/L. AZD5153 efficiently downregulates MYC protein levels across the cell line panel irrespective of their sensitivity to AZD5153. AML, MM, and DLBCL cell lines are highly sensitive to AZD5153. |
| In vivo | AZD5153 modulates MYC and HEXIM1 in AML xenograft tumors and human whole blood. 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 is administered orally to mice bearing MV-4-11 xenografts, and pharmacodynamic activity (intratumoral levels of c-Myc) is measured at 2, 4, and 8 h postdose. A considerable decrease in c-Myc expression is observed out to 8 h post dose at free plasma levels of compound <0.2 μM. This decrease in c-Myc expression after treatment with AZD5153 is consistent with other published BET inhibitors. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (4.94 mM), Sonication is recommended.
Ethanol : 26 mg/mL (38.94 mM), Sonication is recommended.
DMSO : 250 mg/mL (374.39 mM), Sonication is recommended.
|
| Keywords | FL-BRD4 | EpigeneticReaderDomain | Epigenetic Reader Domain | BD1-BRD4 | AZD-5153 HNT | AZD5153 6-Hydroxy-2-naphthoic acid | AZD-5153 6-Hydroxy-2-naphthoic acid | AZD5153 6Hydroxy2naphthoic acid | AZD5153 6 Hydroxy 2 naphthoic acid | AZD-5153 | AZD 5153 |
| Inhibitors Related | ABBV-744 | SNDX-5613 | CeMMEC1 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | (+)-JQ-1 | J-147 | 5-Ph-IAA | Curcumin | dBET6 | Naphthol AS-E | JQ-1 (carboxylic acid) | Bisdemethoxycurcumin |
| Related Compound Libraries | Reprogramming Compound Library | Bioactive Compound Library | Epigenetics Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Orally Active Compound Library | Anti-Aging Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
