MYCMI-6

MYCMI-6

中文名称MYCMI-6
中文同义词3-((9-氨基-7-乙氧基吖啶-3-基)偶氮基)吡啶-2,6-二胺;化合物MYCMI-6
英文名称MYCMI-6
英文同义词MYCMI-6;NSC354961;2,6-Pyridinediamine, 3-[2-(9-amino-7-ethoxy-3-acridinyl)diazenyl]-;MYCMI-6(NSC 354961);3-((9-Amino-7-ethoxyacridin-3-yl)diazenyl)pyridine-2,6-diamine;NSC 354961,cells,neuroblastoma,cytotoxic,mice,tumor,inhibit,nude,lymphoma,MYCMI-6,athymic,Inhibitor,NSC-354961,MYC-driven,Apoptosis,Myc,c-Myc,MYCMI6,MCF7,MYCMI 6
CAS号681282-09-7
分子式C20H19N7O
分子量373.41
EINECS号
相关类别
Mol文件681282-09-7.mol
结构式MYCMI-6 结构式

MYCMI-6 性质

沸点699.5±55.0 °C(Predicted)
密度1.46±0.1 g/cm3(Predicted)
储存条件under inert gas (nitrogen or Argon) at 2–8 °C
酸度系数(pKa)7.53±0.10(Predicted)

MYCMI-6 用途与合成方法

MYCMI-6 (NSC354961) 是一种有效的选择性内源性 MYC:MAX 蛋白相互作用抑制剂。 MYCMI-6 阻断 MYC 驱动的转录。MYCMI-6 选择性结合 MYC bHLHZip 域,Kd 值为 1.6 μM。MYCMI-6 以 MYC 依赖性的方式抑制肿瘤细胞的生长 (IC50<0.5 μM)。MYCMI-6 对正常人细胞无细胞毒性。MYCMI-6 诱导细胞凋亡 (apoptosis)。

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.

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/04/30HY-124675MYCMI-6
MYCMI-6
681282-09-75mg800元
2024/04/30HY-124675MYCMI-6
MYCMI-6
681282-09-710 mg1120元

MYCMI-6 上下游产品信息

"MYCMI-6"相关产品信息
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