MYCMI-6

生物活性体外研究体内研究 MYCMI-6 试剂级价格

MYCMI-6

CAS号:681282-09-7
英文名:MYCMI-6
中文名:MYCMI-6
CBNumber:CB84668251
分子式:C20H19N7O
分子量:373.41
MOL File:681282-09-7.mol

MYCMI-6化学性质

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)
形态 :Solid
颜色 :Brown to reddish brown

MYCMI-6性质、用途与生产工艺

生物活性 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)。

体外研究

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.

体内研究

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.