AZD5153 6-Hydroxy-2-naphthoic acid|cas 1869912-40-2

AZD5153 6-Hydroxy-2-naphthoic acid|cas 1869912-40-2

DC Chemicals, Website: www.dcchemicals.com

Product Name: AZD5153 6-Hydroxy-2-naphthoic acid|Cas Number: 1869912-40-2| Catalog Number: DC10288|Other Nmaes: AZD 5153 6-Hydroxy-2-naphthoic acid; AZD-5153 6-Hydroxy-2-naphthoic acid

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.

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].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].