1. PI3K/Akt/mTOR
    Apoptosis
  2. PI3K
    Apoptosis
  3. SF1126

SF1126 

目录号: HY-10220
产品使用指南

SF1126 是双重 PI3K/BRD4 泛抑制剂,具有抗肿瘤和抗血管生成活性。SF1126 是 RGDS-缀合的 LY294002 前体,其设计为表现出增加的溶解度并与肿瘤区室内的特定整联蛋白结合。SF1126 诱导细胞凋亡 (apoptosis)。

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SF1126 Chemical Structure

SF1126 Chemical Structure

CAS No. : 936487-67-1

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  • 生物活性

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生物活性

SF1126 is a relevant pan and dual first-in-class PI3K/BRD4 inhibitor, has antitumor and anti-angiogenic activity. SF1126 is an RGDS-conjugated LY294002 prodrug, which is designed to exhibit increased solubility and bind to specific integrins within the tumor compartment. SF1126 induces cell apoptosis[1].

IC50 & Target

PI3K/BRD4[1]

体外研究
(In Vitro)

SF1126 (0-6 µM; 48 hours) inhibits Hep3B, HepG2, SK-Hep1, and Huh7 cells proliferation with IC50s of 5.05, 6.89, 3.14, and 2.14 µM, respectively[1].
SF1126 (1-10 µM; 24 hours) results in cell-cycle arrest with a proportional increase in G0-G1 and a decrease in the number of cells in the S-phase in Hep 3B, Hep G2, SK-Hep1, and Huh7 cells[1].
SF1126 (0.5-2.5 µM; pre-30 minutes) and sorafenib suggests that combined treatment of SF1126 and sorafenib blocks multiple key enzymes in PI3K/AKT/mTOR and Ras/Raf/MAPK pathway[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Hep3B, HepG2, SK-Hep1, and Huh7 cells
Concentration: 0 µM; 1 µM; 2 µM; 3 µM; 4 µM; 5 µM; 6 µM
Incubation Time: 48 hours
Result: Resulted in an increased inhibition of HCC proliferation.

Cell Cycle Analysis[1]

Cell Line: Hep3B, HepG2, SK-Hep1, and Huh7 cells
Concentration: 1 µM; 5 µM; 10 µM
Incubation Time: 24 hours
Result: Induced cell-cycle arrest.

Western Blot Analysis[1]

Cell Line: Hep3B, HepG2, SK-Hep1, and Huh7 cells
Concentration: 0.5 µM and 2.5 µM
Incubation Time: Pre-30 mins
Result: Suppressed phosphorylation of AKT, p70S6K, 4EBP1, and ERK in all the cell lines together with sorafenib.
Clinical Trial
分子量

852.84

Formula

C39H48N8O14

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
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  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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