MYCi975 |
カタログ番号GC38588
One-Click Copy Product Info
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MYCi975はc-Mycの小分子阻害剤である。
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はc-Mycの小分子阻害剤である[1]。MYCi975はc-Mycタンパク質に直接結合でき、Maxとのヘテロ二量体形成を遮断し、Thr58におけるc-Mycのリン酸化とタンパク質分解を促進し、よってc-Myc誘導の転写活性と癌細胞増殖を阻害する[2-3]。MYCi975はよく癌の治療に使われる[4]。
HS578T細胞で、MYCi975 (10μM；48時間)の処理は、48時間の培養後、80%に達する細胞のアポトーシスを誘発した[5]。MDA-MB-231細胞で、COTI-2とMYCi975 (0.16-10μM；5日間)の併用処理は、細胞に相乗的な成長阻害効果を示した[6]。A549細胞で、MYCi975 (2.5-10μM；72時間)とTMP269の併用は、NSCLC細胞株の生存率を著しく減らした[7]。
頭頸部扁平上皮癌（HNSCC）ヌードマウスモデルで、MYCi975 (100mg/kg；腹腔内；4週間)の単独投与、またはシスプラチンとの併用処理は、リンパ節の転移を著しく減らした[8]。HNSCC異種移植と同系マウスモデルの両方で、MYCi975(100mg/kg；腹腔内注射；4週間)はHNSCCの成長を阻害した[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.
| 細胞実験[1]: | |
細胞株 | HS578T細胞 |
準備方法 | アポトーシスの測定について、細胞を1ウェルあたり2 × 105の密度で、6ウェルのプレートに播種し、37℃で一晩中培養した。その後、細胞をジメチルスルホキシド（DMSO）または10μM MYCi975で処理した。48時間の培養後、細胞を収穫し、Annexin-V-FITC Apoptosis Detection Kitを使い、アネキシンVとヨウ化プロピジウムで染色した。 |
反応条件 | 10μM；48時間 |
アプリケーション | HS578T細胞で、48時間の培養後、MYCi975の処理は、80%に達する細胞のアポトーシスを誘発した。 |
| 動物実験 [2]: | |
動物モデル | 頭頸部扁平上皮癌（HNSCC）ヌードマウスモデル |
準備方法 | HNSCCの同所性ヌードマウスモデルについて、HNSCC PDXからのEpCAM+ ALDHhigh CSCsをヌードマウスの舌に注射した。注射の1週間後、マウスを四つのグループに分け、下記のものを投与した：1）対照溶媒；2）シスプラチン（体重1kgあたり3mg、1週間）；3）MYCi975 (100mg/kg)；4) MYCi975+シスプラチン、4週間。 |
投与形態 | 100mg/kg；腹腔内注射；4週間 |
アプリケーション | MYCi975の単独投与、またはシスプラチンとの併用は、リンパ節の転移を著しく減らした。 |
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 |
| 溶解度 | 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 | |||
|
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)
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μL
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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.)