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Purity: ≥98%
MCB-613 is a novel and potent stimulator of p160 steroid receptor coactivators (SRCs). It is a Pan-SRCs stimulator. MCB-613 is confirmed to be a strong activator of all three SRCs family proteins. MCB-613 can super-activate transcriptional activity of SRCs. MCB-613 markedly increases SRCs’ interactions with other coactivators. Coactivation of MMP2 or MMP13 promoter-driven luciferase reporter with SRC-3 was greatly enhanced by MCB-613. MCB-613 increased SRC-3’s interaction with CBP and CARM1 robustly in a dose-dependent manner.
| ln Vitro |
In MDA-MB-231 cells, endogenous MMP13 mRNA expression is activated by MCB-613 (6-8 μM; 24 hours)[1]. In 4 hours, MCB-613 (2-10 μM) induces ER stress and proteasome failure. It also phosphorylates eIF2α and IRE1α and increases the expression of the ATF4 protein, which are indicators for the unfolded protein response (UPR)[1]. The viability of SRC-3 KO and WT HeLa cells is impacted by MCB-613 (0-7 μM; 4 hours); SRC-3 WT HeLa cells are more impacted by MCB-613 than KO cells[1].
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| ln Vivo |
When compared to the control group, MCB-613 (intravenous injection; 20 mg/kg; three times/week; seven weeks) markedly and significantly slows the growth of the tumor while posing no clear risk to the animals[1].
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| Cell Assay |
RT-PCR[1]
Cell Types: MDA-MB-231 cells Tested Concentrations: 6 μM; 8 μM Incubation Duration: 24 hrs (hours) Experimental Results: Increased MMP13 mRNA expression. Western Blot Analysis[1] Cell Types: HeLa cells Tested Concentrations: 2 μM; 4 μM; 6 μM; 8 μM; 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: Induced the p-eIF2α, p -IRE1α, and ATF-4 protein expression. Cell Viability Assay[1] Cell Types: SRC-3 KO and WT HeLa cells Tested Concentrations: 3 μM; 4 μM; 5 μM; 6 μM; 7 μM Incubation Duration: 24 hrs (hours) Experimental Results: diminished SRC-3 KO and WT HeLa cell viability. |
| Animal Protocol |
Animal/Disease Models: MCF-7 breast cancer mouse xenograft model (athymic nude mice by injecting MCF-7 cells into mammary fat pads)[1]
Doses: 20 mg/kg Route of Administration: intravenous (iv) injection; 20 mg/kg; 3 times/week; 7 weeks Experimental Results: Inhibited tumor growth in vivo. |
| References |
[1]. Wang L, et al. Characterization of a Steroid Receptor Coactivator Small Molecule Stimulator that Overstimulates Cancer Cells and Leads to Cell Stress and Death. Cancer Cell. 2015 Aug 10;28(2):240-52.
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| Molecular Formula |
C20H20N2O
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| Molecular Weight |
304.39
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| CAS # |
1162656-22-5
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| Related CAS # |
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| SMILES |
O=C1/C(=C(\[H])/C2=C([H])N=C([H])C([H])=C2[H])/C([H])([H])C([H])(C([H])([H])C([H])([H])[H])C([H])([H])/C/1=C(/[H])\C1=C([H])N=C([H])C([H])=C1[H]
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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