512-64-1
中文名稱
醌霉素A
英文名稱
QUINOMYCIN A
CAS
512-64-1
分子式
C51H64N12O12S2
分子量
1101.26
MOL 文件
512-64-1.mol
更新日期
2024/08/21 17:38:37
512-64-1 結(jié)構(gòu)式
基本信息
中文別名
棘霉素醌霉素A
英文別名
SK-302Bnsc526417
NSC 13502
ECHINOMYCIN
QUINOMYCIN A
echinomycina
Echinomycin >97%
Antibiotic A 654I
Echinomycin (NSC-13502)
EchinoMycin, Actinoleukin, 1491, 59266, X 948, X 53III
物理化學(xué)性質(zhì)
熔點217-218℃
比旋光度D20 -310° (c = 0.86 in chloroform)
沸點1427.2±65.0 °C(Predicted)
密度1.0964 (rough estimate)
折射率1.6700 (estimate)
儲存條件-20°C
儲存條件2-8°C
溶解度溶于DMSO（高達5mg/ml）
酸度系數(shù)(pKa)9.38±0.70(Predicted)
形態(tài)白色固體
顏色白色至米色
Merck13,3531
穩(wěn)定性可在-20°C下DMSO溶液中保存長達3個月
安全數(shù)據(jù)
警示詞危險
危險性描述H301+H311+H331-H361
危險品標志T
危險類別碼46-23/24/25
安全說明53-36/37/39-45
危險品運輸編號UN 3462 6.1/PG 2
危險品運輸編號UN 3462 6.1/PG 2
WGK Germany3
WGK Germany3
RTECS號JW5250000
F10
危險等級6.1(b)
包裝類別III
海關(guān)編碼2941900000
常見問題列表
生物活性
Echinomycin (Quinomycin A) 是一種有效的,細胞滲透性的低氧誘導(dǎo)因子-1 (HIF-1) DNA 結(jié)合活性的小分子抑制劑。Echinomycin 選擇性抑制癌癥干細胞，其 IC50 值為 29.4 pM。體外研究
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. |
體內(nèi)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. |