[CAS NO. 1162656-22-5] MCB-613
PRODUCTS SPECIFICATIONS [1162656-22-5]
DESCRIPTION [1162656-22-5]
Overview
| MDL | MFCD01209975 |
|---|---|
| Molecular Weight | 304.39 |
| Molecular Formula | C20H20N2O |
| SMILES | O=C1/C(CC(CC)C/C1=C\C2=CC=CN=C2)=C/C3=CC=CN=C3 |
Summary
MCB-613 is a potent Steroid receptor coactivator SRC small molecule ‘stimulator’ (SMS), super-stimulates SRCs’ transcriptional activity. MCB-613 increases SRCs’ interactions with other coactivators and markedly induces ER stress coupled to the generation of reactive oxygen species ( ROS ). MCB-613 is a SMS that target oncogenes can be exploited as anti-cancer agents by over-stimulating the SRC oncogenic program [1] .
In Vitro
MCB-613 (6-8 μM; 24 hours) activates endogenous MMP13 mRNA expression in MDA-MB-231 cells
[1]
.
MCB-613 (2-10 μM; 4 hours) leads to proteasome dysfunction and ER stress, the induction of the markers for unfolded protein response (UPR), including the phosphorylation of eIF2α and IRE1α as well as the induction of ATF4 protein expression
[1]
.
MCB-613 (0-7 μM; 4 hours) affects SRC-3 KO and WT HeLa cell viability, SRC-3 WT HeLa cell is more affected by MCB-613 compared with KO cells
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
RT-PCR [1]
| Cell Line: | MDA-MB-231 cells |
| Concentration: | 6 μM; 8 μM |
| Incubation Time: | 24 hours |
| Result: | Increased MMP13 mRNA expression. |
Western Blot Analysis [1]
| Cell Line: | HeLa cells |
| Concentration: | 2 μM; 4 μM; 6 μM; 8 μM; 10 μM |
| Incubation Time: | 24 hours |
| Result: | Induced the p-eIF2α, p-IRE1α, and ATF-4 protein expression. |
Cell Viability Assay [1]
| Cell Line: | SRC-3 KO and WT HeLa cells |
| Concentration: | 3 μM; 4 μM; 5 μM; 6 μM; 7 μM |
| Incubation Time: | 24 hours |
| Result: | Decreased SRC-3 KO and WT HeLa cell viability. |
In Vivo
MCB-613 (intravenous injection; 20 mg/kg; 3 times/week; 7 weeks) significantly and dramatically stalls the growth of the tumor compared with the control group and causes no obvious animal toxicity [1]
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | MCF-7 breast cancer mouse xenograft model (athymic nude mice by injecting MCF-7 cells into mammary fat pads) [1] |
| Dosage: | 20 mg/kg |
| Administration: | Intravenous injection; 20 mg/kg; 3 times/week; 7 weeks |
| Result: | Inhibited tumor growth in vivo. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 164.26 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.2853 mL | 16.4263 mL | 32.8526 mL |
| 5 mM | 0.6571 mL | 3.2853 mL | 6.5705 mL |
| 10 mM | 0.3285 mL | 1.6426 mL | 3.2853 mL |