首页Chromatin/EpigeneticEpigenetic Reader DomainAZD5153 6-Hydroxy-2-naphthoic acid
AZD5153 6-Hydroxy-2-naphthoic acid
编号 T3504     别名: AZD-5153 HNT salt, AZD5153
CAS 1869912-40-2     分子式 C25H33N7O3·C11H8O3     分子量 667.75
靶点: BD1-BRD4; FL-BRD4;
AZD 5153 is an orally available, bivalent inhibitor of the bromodomain and extraterminal (BET) protein BRD4 (IC50 = 5 nM). It can simultaneously bind two bromodomains in BRD4, which has been shown to increase antitumor activity in multiple xenograft models of acute myeloid leukemia, multiple myeloma, and diffuse large B cell lymphoma.
纯度:98.2%
规格 库存 单价 数量
2 mg 上海现货 615.00
5 mg 上海现货 1107.00
10 mg 上海现货 1962.00
25 mg 上海现货 3719.00
50 mg 上海现货 7092.00
1 mL * 10 mM (in DMSO) 上海现货 1383.00
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生物活性

产品描述

AZD 5153 is an orally available, bivalent inhibitor of the bromodomain and extraterminal (BET) protein BRD4 (IC50 = 5 nM). It can simultaneously bind two bromodomains in BRD4, which has been shown to increase antitumor activity in multiple xenograft models of acute myeloid leukemia, multiple myeloma, and diffuse large B cell lymphoma.

靶点活性

BD1-BRD4,1.6μM

FL-BRD4,5nM

体外活性

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.

体内活性

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.

细胞实验

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)

细胞系: MV-4-11, MM.1S, and K562 cells

动物实验

动物模型:FeCB17 SCID and SCID beige mice

化学信息

分子量

667.75

分子式

C25H33N7O3·C11H8O3

CAS

1869912-40-2

溶解度

DMSO: 93 mg/mL (139.3 mM)

Ethanol: 26 mg/mL (38.9 mM)

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

store at -80°C

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 1.498 ml 7.488 ml 14.976 ml
5 mM 0.3 ml 1.498 ml 2.995 ml
10 mM 0.15 ml 0.749 ml 1.498 ml
50 mM 0.03 ml 0.15 ml 0.3 ml
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