Molecular Formula | C20H20N2O |
Molar Mass | 304.39 |
Density | 1.159±0.06 g/cm3(Predicted) |
Boling Point | 510.4±50.0 °C(Predicted) |
Solubility | DMSO: 10 mg/mL |
pKa | 4.36±0.12(Predicted) |
Storage Condition | Sealed in dry,Room Temperature |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.285 ml | 16.427 ml | 32.853 ml |
5 mM | 0.657 ml | 3.285 ml | 6.571 ml |
10 mM | 0.329 ml | 1.643 ml | 3.285 ml |
5 mM | 0.066 ml | 0.329 ml | 0.657 ml |
preparation | with 3-pyridinecarboxaldehyde and p-ethylcyclohexanone as raw materials, bipyridine α was obtained by Claisen-Schmidt condensation reaction, Β-unsaturated ketone intermediate 4-ethyl-2, 6-bis (pyridine-3-methylene) cyclohexanone. Dry HCl was used as the catalyst for the condensation reaction. The operation was simple and the yield was over 85%. |
biological activity | MCB-613 is a potent steroid receptor coactivator (SRC) small molecule "stimulators" (SMS), super-stimulate the transcriptional activity of SRCs. MCB-613 increases the interaction of SRC with other co-activators and significantly induces ER stress in combination with the production of reactive oxygen species (ROS). MCB-613 is an SMS that targets oncogenes as anticancer drugs by overstimulating the SRC oncogenic program. |
Cell Line: | MDA-MB-231 cells HeLa cells SRC-3 KO and WT HeLa cells |
Concentration: | 6 μM; 8 μM 2 μM; 4 μM; 6 μM; 8 μM; 10 μM 3 μM; 4 μM; 5 μM; 6 μM; 7 μM |
Incubation Time: | 24 hours 24 hours 24 hours |
Result: | Increased MMP13 mRNA expression. Induced the p-eIF2α, p-IRE1α, and ATF-4 protein expression. Decreased SRC-3 KO and WT HeLa cell viability. Inhibited tumor growth in vivo. |
Animal Model: | MCF-7 breast cancer mouse xenograft model (athymic nude mice by injecting MCF-7 cells into mammary fat pads) |
Dosage: | 20 mg/kg |
Administration: | Intravenous injection; 20 mg/kg; 3 times/week; 7 weeks |