| Identification | Back Directory | [Name]
Mycro3 | [CAS]
944547-46-0 | [Synonyms]
Mycro3
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 | [Molecular Formula]
C24H17ClF2N6O4 | [MDL Number]
MFCD03409284 | [MOL File]
944547-46-0.mol | [Molecular Weight]
526.88 |
| Chemical Properties | Back Directory | [density ]
1.53±0.1 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,Store in freezer, under -20°C | [solubility ]
DMSO : ≥ 100 mg/mL (189.80 mM) | [form ]
Solid | [pka]
6.95±0.46(Predicted) | [color ]
Light yellow to yellow | [InChIKey]
YPPNLSKYXDXQGD-UHFFFAOYSA-N | [SMILES]
N1(C2=CC=CC=C2)C(NC(C2C=C3N(N=2)C(C(Cl)(F)F)=CC(C2=CC=CO2)=N3)=O)=C(C(OCC)=O)C=N1 |
| Hazard Information | Back Directory | [Uses]
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[1]. Mycro 3 could be used for the research of pancreatic cancer[2]. | [Biological Activity]
Mycro 3 is a potent selective Myc-Max dimerization inhibitor. It can be used in pancreatic cancer research. | [in vitro]
Mycro 3 is a potent and selective c-Myc inhibitor in whole cell assays, with weak inhibitory activity against Activator protein 1 (AP-1). It has a superior specificity profile to its predecessors. It inhibits the interaction between c-Myc and Max. It has high selectivity and inhibits c-Myc/Max dimerization and conjugation with DNA. | [in vivo]
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[2]. | Animal Model: | Moribund Pdx1-cre/KRAS* mice bearing pancreatic ductal adenocarcinoma (PDA)[2] | | 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. |
| [target]
| [storage]
Store at -20°C | [References]
[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. DOI:10.7150/ijbs.10190
[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. DOI:10.1093/jnci/dju320 |
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