MYCi975 |
Catalog No.GC38588
One-Click Copy Product Info
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MYCi975 is a small molecule inhibitor of c-Myc.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2289691-01-4
Sample solution is provided at 25 µL, 10mM.
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MYCi975 is a small molecule inhibitor of c-Myc [1]. MYCi975 can directly bind to c-Myc protein, block its heterodimer formation with Max, and promote phosphorylation and protein degradation of c-Myc at Thr58, thereby inhibiting c-Myc-driven transcriptional activity and cancer cell proliferation [2-3]. MYCi975 is commonly used to treat cancer [4].
In HS578T cells, MYCi975 (10μM; 48h) treatment induced apoptosis in up to 80% of cells after 48 h of incubation [5]. In MDA-MB-231 cells, combination treatment of COTI-2 and MYCi975 (0.16-10μM; 5d) produced a synergistic growth inhibitory effect on cells [6]. In A549 cells, combination of MYCi975 (2.5-10μM; 72h) and TMP269 significantly reduced the viability of NSCLC cell lines [7].
In head and neck squamous cell carcinoma (HNSCC) nude mouse model, MYCi975 (100mg/kg; ip; 4 weeks) alone or MYCi975 plus cisplatin significantly reduced lymph node metastasis [8]. In both HNSCC xenograft and syngeneic murine models, MYCi975(100mg/kg; ip; 4 weeks) inhibited HNSCC growth [9].
References:
[1]. Makii R, Ned T, Underdown MJ, et al. 582 A comparative approach to understanding the role of oncogenic MYC signaling in the metastatic osteosarcoma tumor immune microenvironment. Journal of Clinical and Translational Science. 2025 Apr 1; 9(s1): 171.
[2]. Holmes AG, Parker JB, Sagar V, et al. A MYC inhibitor selectively alters the MYC and MAX cistromes and modulates the epigenomic landscape to regulate target gene expression. Science Advances. 2022 Apr 27; 8(17): eabh3635.
[3]. Vízkeleti L, Spisák S. Rewired metabolism caused by the oncogenic deregulation of MYC as an attractive therapeutic target in cancers. Cells. 2023 Jun 29; 12(13): 1745.
[4]. Whitfield JR, Soucek L. MYC in cancer: from undruggable target to clinical trials. Nature Reviews Drug Discovery. 2025 Feb 19: 1-3.
[5]. Tang M, O’Grady S, Crown J, et al. MYC as a therapeutic target for the treatment of triple-negative breast cancer: preclinical investigations with the novel MYC inhibitor, MYCi975. Breast Cancer Research and Treatment. 2022 Sep; 195(2): 105-115.
[6]. Tang M, Crown J, Duffy MJ. Degradation of MYC by the mutant p53 reactivator drug, COTI-2 in breast cancer cells. Investigational New Drugs. 2023 Aug; 41(4):5 41-550.
[7]. Park J, Chen YY, Cao JJ, et al. MYC plus class IIa HDAC inhibition drives mitochondrial dysfunction in non-small cell lung cancer. Cell Reports. 2025 Jun 24; 44(6).
[8]. Liu S, Qin Z, Mao Y, et al. Pharmacological inhibition of MYC to mitigate chemoresistance in preclinical models of squamous cell carcinoma. Theranostics. 2024 Jan 1; 14(2): 622.
[9]. Liu S, Qin Z, Mao Y, et al. Therapeutic targeting of MYC in head and neck squamous cell carcinoma. Oncoimmunology. 2022 Dec 31; 11(1): 2130583.
| Cell experiment [1]: | |
Cell lines | HS578T cells |
Preparation Method | For measuring apoptosis, cells were seeded in 6-well plates at a density of 2 × 105 per well and incubated overnight at 37℃. Cells were then treated with dimethyl sulfoxide (DMSO) or 10μM MYCi975. Following 48h of incubation, they were harvested and stained with annexin-V and propidium iodide using the Annexin-V-FITC Apoptosis Detection Kit. |
Reaction Conditions | 10μM; 48h |
Applications | In HS578T cells, MYCi975 treatment induced apoptosis in up to 80% of cells after 48h of incubation. |
| Animal experiment [2]: | |
Animal models | Head and neck squamous cell carcinoma (HNSCC) nude mouse model |
Preparation Method | For the orthotopic nude mouse model of HNSCC, EpCAM+ ALDHhigh CSCs from HNSCC PDX were injected into the tongues of nude mice. One week after injection, the mice were divided into four groups and given: 1) control vehicle; 2) cisplatin (3mg/kg body weight once a week); 3) MYCi975 (100mg/kg); and 4) MYCi975 plus cisplatin for 4 weeks. |
Dosage form | 100mg/kg; ip; 4 weeks |
Applications | MYCi975 alone or MYCi975 plus cisplatin significantly reduced lymph node metastasis. |
References: | |
| Cas No. | 2289691-01-4 | SDF | |
| Canonical SMILES | OC1=C(C2=CC(C(F)(F)F)=NN2C)C=CC(OCC3=CC=C(Cl)C=C3)=C1C4=CC=C(Cl)C(C(F)(F)F)=C4 | ||
| Formula | C25H16Cl2F6N2O2 | M.Wt | 561.3 |
| Solubility | DMSO: ≥ 250 mg/mL (445.39 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7816 mL | 8.9079 mL | 17.8158 mL |
| 5 mM | 356.3 μL | 1.7816 mL | 3.5632 mL |
| 10 mM | 178.2 μL | 890.8 μL | 1.7816 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)