AZD5153 6-Hydroxy-2-naphthoic acid |
| Catalog No.GC35448 |
AZD5153 6-Hydroxy-2-naphthoic acid는 AZD5153의 6-Hydroxy-2-naphthoic acid입니다. AZD5153은 강력하고 선택적이고 경구로 사용할 수 있는 BET/BRD4 브로모도메인 억제제입니다. 1.7 nM의 IC50으로 BRD4를 파괴합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1869912-40-2
Sample solution is provided at 25 µL, 10mM.
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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. IC50: 1.7 nM (BRD4)[1]
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].
[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.
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