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
- 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.
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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.
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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