AZD5153 6-Hydroxy-2-naphthoic acid

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效、选择性、二价、口服的 BET/BRD4 溴结构域，IC50 为 5 nM。

A potent, selective, bivalent and orally available BET/BRD4 bromodomain with IC50 of 5 nM; simultaneously binds to two bromodomains in BRD4; exhibits antitumor activity in multiple xenograft models of acute myeloid leukemia, multiple myeloma, and diffuse large B cell lymphoma.(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.(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.

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.

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.

AZD 5153 6-Hydroxy-2-naphthoic acid | AZD-5153 6-Hydroxy-2-naphthoic acid

Chromatin/Epigenetic

Bromodomain

BD1-BRD4|FL-BRD4

Cancer

——

1869912-40-2

667.75404

C36H41N7O6

>98% (HPLC)

DMSO: ≥ 34 mg/mL

CC1C(=O)N(CCN1CCOC2=CC=C(C=C2)C3CCN(CC3)C4=NN5C(=NN=C5OC)C=C4)C.C1=CC2=C(C=CC(=C2)O)C=C1C(=O)O

2-Naphthalenecarboxylic acid, 6-hydroxy-, compd. with (3R)-4-[2-[4-[1-(3-methoxy-1,2,4-triazolo[4,3-b]pyridazin-6-yl)-4-piperidinyl]phenoxy]ethyl]-1,3-dimethyl-2-piperazinone (1:1)

(-20℃)

With Ice Pack

≥ 2 years