S87469 |
Mycro 3 |
MedMol | 97% |
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- 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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)