首页Chromatin/EpigeneticEpigenetic Reader DomainMivebresib
Mivebresib
编号 T3712     别名: ABBV-075
CAS 1445993-26-9     分子式 C22H19F2N3O4S     分子量 459.11
靶点: BET;
Mivebresib, also known as ABBV-075, is a potent BET inhibitor (bromodomain (BRD)-containing protein) with potential antineoplastic activity. Upon administration, the bromodomain inhibitor ABBV-075 binds to the acetyl-lysine binding site in the BRD of certain BRD-containing protein(s), thereby preventing the interaction between those proteins and acetylated histones. This disrupts chromatin remodeling, prevents the expression of certain growth-promoting genes, and leads to an inhibition of cell growth in susceptible tumors. Also a potent inhibitor of MYC and the TMPRSS2-ETS fusion proteins.
纯度:98.7%
规格 库存 单价 数量
2 mg 上海现货 774.00
5 mg 上海现货 1012.00
10 mg 上海现货 1819.00
25 mg 上海现货 3719.00
50 mg 上海现货 6712.00
1 mL * 10 mM (in DMSO) 上海现货 1012.00
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生物活性

产品描述

Mivebresib, also known as ABBV-075, is a potent BET inhibitor (bromodomain (BRD)-containing protein) with potential antineoplastic activity. Upon administration, the bromodomain inhibitor ABBV-075 binds to the acetyl-lysine binding site in the BRD of certain BRD-containing protein(s), thereby preventing the interaction between those proteins and acetylated histones. This disrupts chromatin remodeling, prevents the expression of certain growth-promoting genes, and leads to an inhibition of cell growth in susceptible tumors. Also a potent inhibitor of MYC and the TMPRSS2-ETS fusion proteins.

靶点活性

BET,

体外活性

ABBV-075 exhibits robust single agent activity in cell viability assays across cancer cell lines derived from solid tumors, leukemia and lymphomas. It could disrupt cell cycle control leading to G1 arrest followed by senescence, inhibit oncogenesis drivers leading to apoptosis, and potentially target tumor microenvironment to provide additional therapeutic benefit[1].

体内活性

ABBV-075 has comparable or superior efficacies to standard of care agents in flank xenograft mouse models of non-small-cell and small cell lung cancers, pancreatic, breast, prostate, head & neck cancers, multiple myeloma, diffuse large B cell lymphoma and leukemia[1].

化学信息

分子量

459.11

分子式

C22H19F2N3O4S

CAS

1445993-26-9

溶解度

DMSO: 84 mg/mL (183 mM)

Ethanol: <1 mg/mL

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 2.178 ml 10.891 ml 21.781 ml
5 mM 0.436 ml 2.178 ml 4.356 ml
10 mM 0.218 ml 1.089 ml 2.178 ml
50 mM 0.044 ml 0.218 ml 0.436 ml
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