944547-46-0
944547-46-0 結(jié)構(gòu)式
基本信息
C-MYC抑制劑(MYCRO 3)
5-(7-(氯二氟甲基)-5-(呋喃-2-基)吡唑并[1,5-A]嘧啶-2-甲酰胺基)-1-苯基-1H-吡唑-4-羧酸乙酯
Mycro-3, >98%
ethyl 5-[[7-[chloro(difluoro)methyl]-5-(furan-2-yl)pyrazolo[1,5-a]pyrimidine-2-carbonyl]amino]-1-phenylpyrazole-4-carboxylate
1H-Pyrazole-4-carboxylic acid, 5-[[[7-(chlorodifluoromethyl)-5-(2-furanyl)pyrazolo[1,5-a]pyrimidin-2-yl]carbonyl]amino]-1-phenyl-, ethyl ester
物理化學性質(zhì)
常見問題列表
Myc-MAX dimerization
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 IC 50 s of 0.25 and 9.0 μM for cells with intact Myc alleles and Myc-null cells, respectively.
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. |