首页PI3K/Akt/mTOR signalingmTORSF2523
SF2523
编号 T3986    
CAS 1174428-47-7     分子式 C19H17NO5S     分子量 371.41
靶点: BRD4; DNA-PK; mTOR; PI3Kα; PI3Kγ;
SF2523 is a highly selective and potent inhibitor.
纯度:97.8%
规格 库存 单价 数量
1 mg 上海现货 642.00
2 mg 上海现货 1198.00
5 mg 上海现货 2520.00
10 mg 上海现货 4800.00
25 mg 上海现货 8600.00
1 mL * 10 mM (in DMSO) 上海现货 2520.00
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生物活性

产品描述

SF2523 is a highly selective and potent inhibitor.

靶点活性

BRD4,241nM

DNA-PK,9nM

mTOR,280nM

PI3Kα,34nM

PI3Kγ,158nM

体外活性

SF2523 treatment decreases protein levels of MYCN and Cyclin D1, the MYCN target, and inhibits AKT activation by blocking phosphorylation of AKT at Ser473. SF2523 treatment leads to the displacement of BRD4 from both MYCN promoter sites. SF2523 interacts robustly with the full-length BRD4 (Kd=140 nM) and exhibits comparable affinity to the BRD4 first BD (BD1) (Kd=150 nM), however it binds more weakly to the second BD (BD2) of BRD4 (Kd=710 nM). Comparison of binding affinities of SF2523 for BDs of other proteins reveal that it binds equally well to BDs of BRD4, BRD2, and BRD3; shows moderate binding to BDs of CECR2 and BRDT; but associates much weaker with other BDs[1].

体内活性

SF2523 treatment results in a significant reduction of tumor volume compared with control. Importantly, SF2523 shows no gross toxicity to the treated mice, as there is no notable change in body weight. Tumors from SF2523-treated mice have markedly reduced MYCN, pAKT, and Cyclin D1 levels compared with levels of these proteins in vehicle-treated mice tumors[1].

动物实验

动物模型:mice

化学信息

分子量

371.41

分子式

C19H17NO5S

CAS

1174428-47-7

溶解度

DMSO: ≥30 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 2.692 ml 13.462 ml 26.924 ml
5 mM 0.538 ml 2.692 ml 5.385 ml
10 mM 0.269 ml 1.346 ml 2.692 ml
50 mM 0.054 ml 0.269 ml 0.538 ml
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