CAS NO: | 1162656-22-5 |
规格: | ≥98% |
包装 | 价格(元) |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
1g | 电议 |
Molecular Weight (MW) | 304.39 |
---|---|
Formula | C20H20N2O |
CAS No. | 1162656-22-5 |
Storage | -20℃ for 3 years in powder form |
-80℃ for 2 years in solvent | |
Solubility (In vitro) | DMSO: 60 mg/mL (197.1 mM) |
Water: <1 mg/mL | |
Ethanol: 60 mg/mL (197.1 mM) | |
Solubility (In vivo) | 4% DMSO+30% PEG 300+ddH2O: 2mg/mL |
Synonyms | MCB-613; MCB 613; MCB613 |
In Vitro | In vitro activity: MCB-613 selectively and reversibly binds to the RID of SRC-3, and selectively kills cancer cells including MCF-7 (breast), PC-3 (prostate), H1299 (lung), and HepG2 (liver) cells, without toxicity to mouse primary hepatocytes and mouse embryonic fibroblasts (MEFs). MCB-613 also increases SRCs’ interactions with other coactivators and markedly induces ER stress coupled to the generation of reactive oxygen species (ROS). Kinase Assay: After various compound treatments, cells are lysed in luciferase lysis buffer and assayed for luciferase activity using the ONE-Glo luciferase assay system. All luciferase activities are normalized to protein concentration determined by Bradford assay. Cell Assay: Cells [MCF-7 (breast), PC-3 (prostate), H1299 (lung), and HepG2 (liver) cells; mouse primary hepatocytes and mouse embryonic fibroblasts] are seeded in 96-well plates and allowed to reach 60% to 70% confluence. After indicated compound treatments, relative numbers of viable cells are measured by MTS assay using the Cell Titer 96 Aqueous One Solution Cell Proliferation Assay. |
---|---|
In Vivo | In an MCF-7 breast cancer mouse xenograft model, MCB-613 (20 mg/kg, i.p.) significantly and dramatically inhibits the growth of the tumor while causing no obvious animal toxicity and body weight less. |
Animal model | Mice bearing MCF-7 xenografts |
Formulation & Dosage | Dissolved in saline;20 mg/kg; i.p. injection |
References | Cancer Cell. 2015 Aug 10;28(2):240-52 |