681282-09-7
681282-09-7 結(jié)構(gòu)式
基本信息
3-((9-氨基-7-乙氧基吖啶-3-基)偶氮基)吡啶-2,6-二胺
3-[(9-氨基-7-乙氧基吖啶-3-基)二氮烯基]吡啶-2,6-二胺
NSC354961
MYCMI-6(NSC 354961)
2,6-Pyridinediamine, 3-[2-(9-amino-7-ethoxy-3-acridinyl)diazenyl]-
物理化學(xué)性質(zhì)
常見問題列表
MYCMI-6 (NSC354961) (6.25?μM; 48 hours) selectively suppresses MYC-driven tumor cell growth with high efficacy.
MYCMI-6 significantly inhibits growth of Burkitt’s lymphoma cells (Mutu, Daudi and ST486) - another classical example of a MYC-driven tumor, having translocations of
MYC
to one of the immunoglobulin loci - in a dose-dependent manner with an average GI
50
of 0.5?μM. Treatment of MCF7 cells with the MYCMI-6 for 24?hours significantly decreased MYC:MAX isPLA signals to 7%. Titration showed an IC
50
for inhibition of MYC:MAX of less than 1.5?μM for MYCMI-6 by isPLA. MYCMI-6 inhibits the MYC:MAX heterodimer formation with an IC
50
of 3.8?μM. MYCMI-6 efficiently inhibits anchorage-independent growth of
MYCN
-amplified neuroblastoma cells with GI
50
values of <0.4?μM.
Cell Viability Assay
| 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. |
MYCMI-6 (20?mg/kg; i.p.; daily for 1-2 weeks) induces massive apoptosis and reduces tumor cell proliferation, tumor microvasculature density and MYC:MAX interaction in a MYC-dependent xenograft tumor model.
| 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 |
| Result: | 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. |