MYCi975
目录号 : GC38588
MYCi975是一种c-Myc小分子抑制剂。
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.
MYCi975是一种c-Myc小分子抑制剂 [1]。MYCi975可以直接结合c-Myc蛋白，阻断其与Max形成异二聚体，并促进c-Myc在Thr58位点的磷酸化和蛋白质降解，从而抑制c-Myc 驱动的转录活性和癌细胞增殖 [2-3]。MYCi975常用于治疗癌症 [4]。
在HS578T细胞中，MYCi975（10μM；48h）处理48h后，诱导高达80%的细胞凋亡 [5]。在MDA-MB-231细胞中，COTI-2和MYCi975（0.16-10μM；5d）联合处理对细胞产生协同生长抑制作用 [6]。在A549细胞中，MYCi975（2.5-10μM；72h）与TMP269联合应用显著降低了非小细胞肺癌（NSCLC）细胞系的活力 [7]。
在头颈部鳞状细胞癌（HNSCC）裸鼠模型中，MYCi975（100mg/kg；ip；4周）单独给药或MYCi975联合顺铂给药均显著降低了淋巴结转移 [8]。在HNSCC异种移植和同基因小鼠模型中，MYCi975（100mg/kg；ip；4周）均抑制了HNSCC的生长 [9]。
| 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 | ||
| 分子式 | C25H16Cl2F6N2O2 | 分子量 | 561.3 |
| 溶解度 | DMSO: ≥ 250 mg/mL (445.39 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7816 mL | 8.9079 mL | 17.8158 mL |
| 5 mM | 0.3563 mL | 1.7816 mL | 3.5632 mL |
| 10 mM | 0.1782 mL | 0.8908 mL | 1.7816 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet