MYCMI-7 hydrobromide
Based on 1 Customer Validation
MYCMI-7 hydrobromide is a potent and selective MYC/MYCN inhibitor, with a Kd of 4 μM for MYC and an IC50 of 10 μM for topoisomerase IIα (Topoisomerase IIα). MYCMI-7 hydrobromide binds directly to MYC, selectively inhibits the interactions of MYC:MAX and MYCN:MAX, reduces MYC-driven transcription levels, induces MYC/MYCN protein degradation, and blocks the binding of MYC to chromatin, thereby inducing tumor cell growth arrest, apoptosis and reducing cell viability, while only inducing G1 phase growth arrest in normal cells. MYCMI-7 hydrobromide can be used in research related to MYC-driven acute myeloid leukemia and breast cancer, MYCN-amplified neuroblastoma, glioblastoma, Burkitt's lymphoma, melanoma, colon cancer, osteosarcoma, cervical cancer and histiocytic lymphoma.
For research use only. We do not sell to patients.
- Purity : 95.22%
- CAS No.: 102537-38-2
- Formula: C23H28N3·1/2HBr·Br
- Molecular Weight:466.84
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
topoisomerase II alpha 10 μM (IC50) |
MYC 4 μM (Kd) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | GI50 |
5.800 μM
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Antiproliferative activity against human MDA-MB-231 breast cancer cells transfected with control siRNA assessed as reduction in cell viability incubated for unspecified time by resazurin assay.
Antiproliferative activity against human MDA-MB-231 breast cancer cells transfected with control siRNA assessed as reduction in cell viability incubated for unspecified time by resazurin assay.
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36874405 |
| MDA-MB-231 | GI50 |
5.763 μM
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Antiproliferative activity against human MDA-MB-231 breast cancer cells transfected with Top2α-targeting siTOP2A-1 assessed as reduction in cell viability incubated for unspecified time by resazurin assay.
Antiproliferative activity against human MDA-MB-231 breast cancer cells transfected with Top2α-targeting siTOP2A-1 assessed as reduction in cell viability incubated for unspecified time by resazurin assay.
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36874405 |
| MDA-MB-231 | GI50 |
5.803 μM
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Antiproliferative activity against human MDA-MB-231 breast cancer cells transfected with Top2α-targeting siTOP2A-2 assessed as reduction in cell viability incubated for unspecified time by resazurin assay.
Antiproliferative activity against human MDA-MB-231 breast cancer cells transfected with Top2α-targeting siTOP2A-2 assessed as reduction in cell viability incubated for unspecified time by resazurin assay.
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36874405 |
| MDA-MB-231 | GI50 |
5.491 μM
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Antiproliferative activity against untreated human MDA-MB-231 breast cancer cells assessed as reduction in cell viability incubated for unspecified time by resazurin assay.
Antiproliferative activity against untreated human MDA-MB-231 breast cancer cells assessed as reduction in cell viability incubated for unspecified time by resazurin assay.
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36874405 |
In Vitro
MYCMI-7 hydrobromide (0.5-10 μM; 72 h) induces growth arrest in normal human skin fibroblasts without reducing cell viability[1].
MYCMI-7 hydrobromide (1-100 μM; 10 min) potently inhibits the decatenation activity of recombinant human Top2α in cell-free assays[1].
MYCMI-7 hydrobromide (5 μM; 6 h) blocks the binding of MYC to the promoter of the ODC1 target gene in U-937 cells[1].
MYCMI-7 (1-6 h) hydrobromide reduces the formation of MYC:MAX complex and the expression of MYC protein in MCF7 cells in a time-dependent manner[1].
MYCMI-7 hydrobromide (5 μM; 17 h) downregulates the protein expression of MYC, MYCN, phosphorylated MYC, and MAX in MCF7, HeLa, Kelly, P493-6, HCT116, and neuroblastoma cell lines, and reduces the steady-state levels of wild-type and mutant MYC in U2OS cells[1].
MYCMI-7 (10-30 μM; 96 h) hydrobromide reduces the growth of H015.19 Rat1 fibroblasts in a concentration-dependent manner[1].
MYCMI-7 (0.1-6.25 μM; 2 h-2 weeks) hydrobromide inhibits anchorage-independent growth of SK-N-DZ MYCN-amplified neuroblastoma cells, potently reduces the growth capacity of MYC-translocated Daudi, Raji and Mutu Burkitt lymphoma cells after 24 hours, and strongly decreases anchorage-independent colony formation of MYC+HRAS-transformed primary REF[1].
MYCMI-7 hydrobromide reduces the growth of MDA-MB-231 cells with a GI50 of approximately 5.5-5.8 μM, and knockdown of Top2α does not alter the sensitivity of cells to MYCMI-7[1].
MYCMI-7 (0.5-12 μM; 72 h) hydrobromide potently inhibits the growth/activity of AML cells driven by MYC/BCL-XL, and suppresses the growth of MDA-MB-231 breast cancer cells in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MCF7, HeLa, P493-6, HCT116, Kelly, SK-N-DZ, CHP212, SK-N-AS, U2OS human cancer and fibroblast cell lines
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Concentration:5 μM
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Incubation Time:17 h; overnight (U2OS cells, post-24 h transfection)
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Result:Reduced MYC protein expression in MCF7, HeLa, P493-6, wild-type HCT116, and FBW7-/- HCT116 cells.
Reduced MYCN protein expression in Kelly neuroblastoma cells.
Reduced phosphorylated MYC and total MYC expression in FBW7-/- HCT116 cells to ~75% of DMSO control levels.
Reduced steady-state levels of wild-type and T58A/S62A mutant MYC in U2OS cells.
Reduced MAX protein expression in Kelly, SK-N-DZ, CHP212, and SK-N-AS neuroblastoma cells.
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Cell Line:H015.19 Rat1 fibroblasts (MYC-proficient)
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Concentration:10, 20, 30 μM
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Incubation Time:96 h
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Result:Reduced cell growth/viability to ~90% at 10 μM, ~45% at 20 μM, and ~25% at 30 μM relative to DMSO control.
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Cell Line:Daudi, Raji, and Mutu Burkitt's lymphoma cells (MYC-translocated)
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Concentration:6.25 μM
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Incubation Time:24 h
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Result:Reduced cell growth/viability to ~18% in Daudi cells, ~25% in Raji cells, and ~18% in Mutu cells relative to DMSO control.
All reductions showed statistically significant differences (p<0.01 to p<0.05).
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Cell Line:MYC/BCL-XL-driven acute myeloid leukemia (AML) cells
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Concentration:0, 0.5, 1, 2, 3, 4, 5, 6, 7, 8 μM
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Incubation Time:72 h
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Result:Reduced cell growth/viability in a concentration-dependent manner.
Achieved complete inhibition at concentrations ≥3 μM.
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Cell Line:MDA-MB-231 human breast cancer cells
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Concentration:0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12 μM
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Incubation Time:72 h
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Result:Reduced cell growth/viability in a concentration-dependent manner.
Achieved near-complete inhibition at 10 μM.
In Vivo
MYCMI-7 (6.25 mg/kg; i.t.; twice weekly; 26 days) hydrobromid einhibits the growth of MDA-MB-231 breast cancer xenografts, reduces MYC expression levels, induces cell apoptosis, and significantly improves the survival rate of mice[1].
MYCMI-7 (6.25 mg/kg; i.t.; twice weekly; 20 days) hydrobromide inhibits the growth of MYCN-amplified SK-N-DZ neuroblastoma xenografts, reduces MYCN expression, and significantly improves the survival rate of mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL mice (sublethally irradiated)[1]
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Dosage:12.5 mg/kg
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Administration:i.p.; once daily; 15 days
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Result:Reduced GFP+ leukemic cells in bone marrow from ~4% to undetectable levels at day 15.
Reduced GFP+ leukemic cells in bone marrow from ~40% to ~10% at endpoint.
Significantly reduced MYC expression in leukemic spleen cells.
Increased cleaved caspase-3 and H3K9me3 expression in leukemic spleens.
Showed no significant difference in overall survival between groups.
Retained body weight with no severe side effects.
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Animal Model:NOD/SCID mice (6-8 weeks old)[1]
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Dosage:6.25 mg/kg
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Administration:i.t.; twice weekly; 26 days
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Result:Significantly slowed tumor growth, with a significant difference in tumor volume observed at day 11.
Significantly increased mouse survival.
Induced extensive necrosis/apoptosis in tumor tissue.
Reduced MYC expression in tumor tissue.
Increased cleaved caspase-3 and TUNEL staining in tumor tissue.
Reduced Ki67 staining (proliferation) in tumor tissue.
Reduced CD31 staining (microvascular density) in tumor tissue.
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Animal Model:NMRI nu/nu mice (6-8 weeks old)[1]
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Dosage:6.25 mg/kg
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Administration:i.t.; twice weekly; 30 days
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Result:Reduced tumor growth, with a significant difference in tumor volume observed at day 7.
Significantly increased mouse survival.
Induced massive apoptosis/necrosis and hemorrhage in tumor tissue.
Strongly reduced MYCN expression in tumor tissue.
Chemical Information
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CAS No. 102537-38-2
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Appearance Solid
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Molecular Weight 466.84
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Formula C23H28N3·1/2HBr·Br
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Color Light yellow to yellow
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SMILES
CC1=C(C2=C(C)C3=C1C=C[N+](CCN(CC)CC)=C3)NC4=C2C=CC=C4.[Br-].Br.[1/2]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 33.33 mg/mL (71.39 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3.33 mg/mL (7.13 mM); Clear solution
This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3.33 mg/mL (7.13 mM); Clear solution
This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Somatic Cell Culture
A method of simulating the in vivo environment in vitro to maintain the cell growth, differentation and main functions.
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CCK-8/WST-8 Cell Proliferation Assay
The CCK-8/WST-8 assay is based on the reduction of the water-soluble tetrazolium salt WST-8 to a water-soluble formazan product by cellular dehydrogenases in metabolically active cells, where the generated formazan amount is proportional to the number of living cells and is quantified by measuring absorbance in the visible range, providing a colorimetric readout for cell viability and proliferation assessment. This class of tetrazolium-based assays improves upon earlier MTT-based systems by producing a water-soluble formazan, eliminating the need for organic solubilization steps and enabling direct spectrophotometric measurement in culture medium.
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Cell Counting-Based Growth Curve Assay
Cell counting-based growth curve assays quantify cell proliferation by directly measuring changes in viable cell number over time using manual or automated counting methods such as hemocytometer-based counting or instrument-assisted cell enumeration, enabling construction of growth curves that reflect population expansion dynamics in response to culture conditions. A widely used approach is trypan blue exclusion with hemocytometer counting, where membrane-compromised (non-viable) cells take up the dye, allowing discrimination between viable and non-viable cells while simultaneously enabling total cell number quantification. Repeated sampling across time points allows estimation of proliferation rate, growth phases, and comparative growth kinetics between experimental conditions.
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
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Detection of Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Protocol for Cell Counting and Cell Density Analysis
Cell counting and cell-density analysis estimate the number of cells in a known volume or field area. Manual hemocytometer counting uses a chamber of defined geometry to convert counted cells into cells/mL, while automated counters and image-analysis workflows detect cell objects from optical, brightfield, fluorescence, impedance, or digital-image features. Trypan blue viability counting is based on dye exclusion: viable cells with intact membranes exclude dye, while non-viable cells with compromised membranes stain blue. The readout is total cell density, viable-cell density, dead-cell density, and percent viability. Cell density can also be estimated from microscopy images by counting objects per image area, from flow cytometry using calibrated volume or reference particles, or from in situ microscopy in bioreactors after calibration against reference methods such as hemocytometer or flow cytometry.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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MTT Cell Proliferation Assay
The MTT assay is a colorimetric endpoint assay for estimating viable cell number, cell growth, cytotoxicity, or cell activation in cultured mammalian cells. Living cells reduce the yellow tetrazolium salt MTT into purple/blue formazan, while dead cells do not generate the same signal; the resulting color can be quantified with a multiwell spectrophotometer. MTT reduction is commonly interpreted as a readout of metabolic activity that often correlates with viable cell number, but it should not be treated as a direct cell-counting method unless the assay is optimized for the cell type and experimental condition. Studies show that MTT reduction can involve mitochondrial and non-mitochondrial reducing systems, and formazan may accumulate in intracellular lipid droplets rather than simply marking mitochondria.
Purity & Documentation
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Data Sheet (294 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1421 mL | 10.7103 mL | 21.4206 mL | 53.5515 mL |
| 5 mM | 0.4284 mL | 2.1421 mL | 4.2841 mL | 10.7103 mL | |
| 10 mM | 0.2142 mL | 1.0710 mL | 2.1421 mL | 5.3552 mL | |
| 15 mM | 0.1428 mL | 0.7140 mL | 1.4280 mL | 3.5701 mL | |
| 20 mM | 0.1071 mL | 0.5355 mL | 1.0710 mL | 2.6776 mL | |
| 25 mM | 0.0857 mL | 0.4284 mL | 0.8568 mL | 2.1421 mL | |
| 30 mM | 0.0714 mL | 0.3570 mL | 0.7140 mL | 1.7851 mL | |
| 40 mM | 0.0536 mL | 0.2678 mL | 0.5355 mL | 1.3388 mL | |
| 50 mM | 0.0428 mL | 0.2142 mL | 0.4284 mL | 1.0710 mL | |
| 60 mM | 0.0357 mL | 0.1785 mL | 0.3570 mL | 0.8925 mL |
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