醌霉素A

生物活性体外研究体内研究醌霉素A 试剂级价格

醌霉素A

CAS号:512-64-1
英文名:QUINOMYCIN A
中文名:醌霉素A
CBNumber:CB6394145
分子式:C51H64N12O12S2
分子量:1101.26
MOL File:512-64-1.mol

醌霉素A化学性质

熔点 :217-218℃
比旋光度 :D20 -310° (c = 0.86 in chloroform)
沸点 :1427.2±65.0 °C(Predicted)
密度 :1.0964 (rough estimate)
折射率 :1.6700 (estimate)
储存条件 :-20°C
溶解度 :Soluble in DMSO (up to 5 mg/ml)
酸度系数(pKa) :9.38±0.70(Predicted)
形态 :White solid
颜色 :white to beige
Merck :13,3531
稳定性 :Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months

安全信息

危险品标志 :T
危险类别码 :46-23/24/25
安全说明 :53-36/37/39-45
危险品运输编号 :UN 3462 6.1/PG 2
WGK Germany :3
RTECS号 :JW5250000
F :10
危险等级 :6.1(b)
包装类别 :III
海关编码 :2941900000

醌霉素A性质、用途与生产工艺

生物活性 Echinomycin (Quinomycin A) 是一种有效的,细胞渗透性的低氧诱导因子-1 (HIF-1) DNA 结合活性的小分子抑制剂。Echinomycin 选择性抑制癌症干细胞，其 IC50 值为 29.4 pM。

体外研究

Echinomycin (0-10 nM; 16 hours; U251 cells) treatment significantly inhibits hypoxia-induced VEGF mRNA expression in a dose-dependent fashion. Echinomycin very potently inhibits hypoxic induction of luciferase expression in U251-HRE in a dose-dependent fashion with an EC ₅₀ of 1.2 nM.

RT-PCR

Cell Line:	U251 cells
Concentration:	0 nM, 0.625 nM, 1.25 nM, 5 nM, 10 nM
Incubation Time:	16 hours
Result:	Significantly inhibited VEGF mRNA expression induced by hypoxia in a dose-dependent fashion.

体内研究

Echinomycin (10 μg/kg; intravenous injection; for 40 days; NOD-SCID mice) treatment efficiently eradicates mouse lymphoma and serially transplantable human acute myeloid leukemia (AML) in xenogeneic model by preferential elimination of cancer stem cells (CSCs). HIF1α maintains mouse lymphoma CSCs by repressing a negative feedback loop in the Notch pathway.

Animal Model:	NOD-SCID mice received 1.8Gy of irradiation and i.v. injection with peripheral blood cells from patients AML-71 and AML-150
Dosage:	10 μg/kg
Administration:	Intravenous injection; for 40 days
Result:	Efficiently eradicated mouse lymphoma and serially transplantable human AML in xenogeneic model by preferential elimination of CSCs.