Name | MYCMI-6 |
Synonyms | MYCMI-6 NSC354961 MYCMI-6(NSC 354961) 3-((9-Amino-7-ethoxyacridin-3-yl)diazenyl)pyridine-2,6-diamine 2,6-Pyridinediamine, 3-[2-(9-amino-7-ethoxy-3-acridinyl)diazenyl]- |
CAS | 681282-09-7 |
Molecular Formula | C20H19N7O |
Molar Mass | 373.41 |
Density | 1.46±0.1 g/cm3(Predicted) |
Boling Point | 699.5±55.0 °C(Predicted) |
pKa | 7.53±0.10(Predicted) |
Storage Condition | under inert gas (nitrogen or Argon) at 2–8 °C |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.678 ml | 13.39 ml | 26.78 ml |
5 mM | 0.536 ml | 2.678 ml | 5.356 ml |
10 mM | 0.268 ml | 1.339 ml | 2.678 ml |
5 mM | 0.054 ml | 0.268 ml | 0.536 ml |
biological activity | MYCMI-6 (NSC354961) is a potent and selective inhibitor of endogenous MYC:MAX protein interactions. MYCMI-6 blocking MYC-driven transcription. MYCMI-6 selectively binds to MYC bHLHZip domain with a Kd value of 1.6 μm. MYCMI-6 inhibited tumor cell growth in a MYC-dependent manner (IC50<0.5 μm). MYCMI-6 to normal human cells without cytotoxicity. MYCMI-6 induced apoptosis (apoptosis). |
Cell Line: | MYCN -amplified neuroblastoma cells (IMR-32, Kelly and SK-N-DZ), MYCN -non-amplified neuroblastoma cells (SK-N-F1, SK-N-AS and SK-N-RA) |
Concentration: | 6.25 μM |
Incubation Time: | 48 hours |
Result: | Reduced growth of the MYCN -amplified cell lines significantly stronger than the MYCN -non-amplified cell lines. A dramatic increase in the extension of apoptotic areas in the tumors and a significant increase in non-proliferative areas as determined by Ki67 staining in tumors. |
Animal Model: | 6-8 weeks old athymic nude mice (bearing MYCN-amplified SK-N-DZ neuroblastoma cells) |
Dosage: | 20 mg/kg body weight |
Administration: | I.p.; daily for 1-2 weeks |