首页Chromatin/EpigeneticEpigenetic Reader DomainINCB057643
INCB057643
编号 T5417    
CAS 1820889-23-3     分子式 C20H21N3O5S     分子量 415.46
靶点: BET;
INCB057643 is a potent, selective and orally bioavailable BET inhibitor.
纯度:98.70%
规格 库存 单价 数量
2 mg 上海现货 1012.00
5 mg 上海现货 1772.00
10 mg 上海现货 3007.00
25 mg 上海现货 5412.00
50 mg 上海现货 7576.00
1 mL * 10 mM (in DMSO) 上海现货 1772.00
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生物活性

产品描述

INCB057643 is a potent, selective and orally bioavailable BET inhibitor.

靶点活性

BET,

体外活性

INCB057643 inhibited binding of BRD2/BRD3/BRD4 to an acetylated histone H4 peptide in the low nM range and was selective against other bromodomain-containing proteins. INCB057643 inhibited proliferation of human AML, DLBCL, and multiple myeloma cell lines, with a corresponding decrease in MYC protein levels. Cell cycle analyses indicated that G1 arrest and a concentration-dependent increase in apoptosis were seen within 48 hours of treatment with INCB057643. BRD proteins also regulate the expression of many pro-inflammatory genes. Production of several cytokines, including IL-6, IL-10 and MIP-1α, was repressed by INCB057643 in human and mouse whole blood stimulated ex vivo with LPS [1].

体内活性

Oral administration of INCB057643 resulted in significant anti-tumor efficacy in xenograft models of AML, myeloma, and DLBCL. Additionally, combining INCB057643 with the standard of care agents used for the treatment of DLBCL including rituximab and bendamustine resulted in enhanced anti-tumor efficacy relative to that achieved with single-agent therapies at doses that were well tolerated [1].

化学信息

分子量

415.46

分子式

C20H21N3O5S

CAS

1820889-23-3

溶解度

DMSO: 60 mg/mL (144.42 mM)

( < 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 2.407 ml 12.035 ml 24.07 ml
5 mM 0.481 ml 2.407 ml 4.814 ml
10 mM 0.241 ml 1.203 ml 2.407 ml
50 mM 0.048 ml 0.241 ml 0.481 ml
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