产品描述: | Mycro 3 is an orally active, potent and selective inhibitor of Myc-associated factor X (MAX) dimerization. Mycro 3 also inhibit DNA binding of c-Myc. Mycro 3 could be used for the research of pancreatic cancer |
靶点: |
Myc-MAX dimerization;c-Myc; Autophagy |
体外研究: |
Mycro 3 is a potent and selective c-Myc inhibitor in whole cell assays, with weak inhibitory activity against Activator protein 1 (AP-1). Mycro 3 has a superior specificity profile to its predecessors. Mycro 3 inhibits the interaction between c-Myc and Max. Mycro 3 has high selectivity and inhibits c-Myc/Max dimerization and conjugation with DNA. Mycro 3 exhibits an excellent specificity with IC50s of 0.25 and 9.0 µM for cells with intact Myc alleles and Myc-null cells, respectively |
体内研究: |
Mycro 3 (100 mg/kg; oral administration; daily for two months) induces marked shrinkage of pancreatic ductal adenocarcinoma (PDA), increases cancer cell apoptosis, and reduces cell proliferation. Tumor growth is also drastically attenuated in Mycro 3-treated NOD/SCID mice carrying orthotopic or heterotopic xenografts of human pancreatic cancer cells. Animal Model: Moribund Pdx1-cre/KRAS* mice bearing pancreatic ductal adenocarcinoma (PDA) Dosage: 100 mg/kg Administration: Oral administration; daily for two months Result: Increased survival time.Mycro 3 administration was discontinued after two months, the mouse survived for an additional month. |
参考文献: |
1. Chen BJ, et al. Small molecules targeting c-Myc oncogene: promising anti-cancer therapeutics. Int J Biol Sci. 2014 Sep 13;10(10):1084-96. 2. Dimitris Stellas, et al. Therapeutic effects of an anti-Myc drug on mouse pancreatic cancer. J Natl Cancer Inst. 2014 Oct 11;106(12):dju320. |
溶解性: |
Soluble in DMSO |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
1.898 ml |
9.49 ml |
18.98 ml |
5 mM |
0.38 ml |
1.898 ml |
3.796 ml |
10 mM |
0.19 ml |
0.949 ml |
1.898 ml |
50 mM |
0.038 ml |
0.19 ml |
0.38 ml |
|
注意: |
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