944547-46-0
| 中文名称 | 944547-46-0 |
|---|---|
| 中文同义词 | C-MYC抑制剂(MYCRO 3);化合物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 |
| 英文名称 | Mycro3 |
| 英文同义词 | Mycro3;ethyl 5-[[7-[chloro(difluoro)methyl]-5-(furan-2-yl)pyrazolo[1,5-a]pyrimidine-2-carbonyl]amino]-1-phenylpyrazole-4-carboxylate;Mycro-3, >98%;1H-Pyrazole-4-carboxylic acid, 5-[[[7-(chlorodifluoromethyl)-5-(2-furanyl)pyrazolo[1,5-a]pyrimidin-2-yl]carbonyl]amino]-1-phenyl-, ethyl ester;Ethyl 5-(7-(chlorodifluoromethyl)-5-(furan-2-yl)pyrazolo[1,5-a]pyrimidine-2-carboxamido)-1-phenyl-1H-pyrazole-4-carboxylate;dimerization,Mycro 3,pancreatic,inhibit,adenocarcinoma,ductal,c-Myc,Inhibitor,PDA,Autophagy,Mycro3,MAX,Myc |
| CAS号 | 944547-46-0 |
| 分子式 | C24H17ClF2N6O4 |
| 分子量 | 526.88 |
| EINECS号 | |
| 相关类别 | 细胞生物学试剂 |
| Mol文件 | 944547-46-0.mol |
| 结构式 |  |
944547-46-0 性质
| 密度 | 1.53±0.1 g/cm3(Predicted) |
|---|---|
| 储存条件 | Sealed in dry,Store in freezer, under -20°C |
| 溶解度 | 二甲基亚砜：≥100mg/mL（189.80mM） |
| 酸度系数(pKa) | 6.95±0.46(Predicted) |
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. |