DHAQ DIACETATE

DHAQ DIACETATE用途

米托蒽醌二乙酸酯是一种有效的拓扑异构酶II抑制剂。米托蒽醌二乙酸酯也抑制蛋白激酶C(PKC)活性,IC50为8.5μM。米托蒽醌二乙酸酯诱导B-CLL(B-慢性淋巴细胞白血病)细胞凋亡。米托蒽醌二乙酸酯具有抗肿瘤活性[1][2][3][4]。米托蒽醌二乙酸酯还具有抗正痘病毒活性,EC50分别为0.25μM和0.8μM,用于牛痘和猴痘[5]。

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DHAQ DIACETATE名称

[ CAS 号 ]:
70711-41-0

[ 英文名 ]:
DHAQ DIACETATE

DHAQ DIACETATE生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 表观遗传学 >> PKC

信号通路 >> 细胞凋亡 >> 细胞凋亡

信号通路 >> 细胞周期/DNA损伤 >> 拓扑异构酶

信号通路 >> TGF-beta/Smad 信号通路 >> PKC

[ 靶点 ]

IC50: 8.5 μM (PKC)[1]

[体外研究]

米托蒽醌二乙酸酯以与组蛋白H1竞争的方式抑制PKC,其Ki值为6.3μM,并以与磷脂酰丝氨酸和ATP非竞争的方式[1]。米托蒽醌二乙酸酯(0.5μg/mL,48小时)诱导B-CLL细胞减少。米托蒽醌二乙酸酯诱导DNA片段化和聚ADP核糖聚合酶(PARP)的蛋白水解裂解,表明米托蒽酮二乙酸酯的细胞毒性作用是由于诱导细胞凋亡[2]。米托蒽醌二乙酸酯对人乳腺癌细胞系MDA-MB-231和MCF-7具有细胞毒性,IC50值分别为18和196 nM[3]。

[体内研究]

米托蒽醌二醋酸盐(IP,0-3.2毫克/千克/天)在IP植入L1210白血病的小鼠中以1.6毫克/千克产生具有统计学意义的60天存活人数[4]。米托蒽醌二乙酸酯(IV,0-3.2 mg/kg/天)在SC植入的Lewis肺癌中显示出有效的抗肿瘤活性,并在3.2毫克/千克时产生60%的ILS(寿命延长)[4]。

DHAQ DIACETATE物理化学性质

[ 密度 ]:
1.45g/cm3

[ 沸点 ]:
805.7ºC at 760 mmHg

[ 熔点 ]:
203-5ºC

[ 分子式 ]:
C₂₄H₃₂N₄O₈

[ 分子量 ]:
504.53300

[ 闪点 ]:
441.1ºC

[ 精确质量 ]:
504.22200

[ PSA ]:
200.48000

[ LogP ]:
0.87950

DHAQ DIACETATE毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: CB5749000

CHEMICAL NAME :: Anthraquinone, 5,8-bis((2-((2-hydroxyethyl)amino)ethyl)amino)-1,4-di hydroxy-, 1,4-diacetate (salt)

CAS REGISTRY NUMBER :: 70711-41-0

LAST UPDATED :: 199410

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C22-H28-N4-O6.2C2-H4-O2

MOLECULAR WEIGHT :: 564.66

WISWESSER LINE NOTATION :: L C666 BV IVJ DOV1 GOV1 KM2M2Q NM2M2Q

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 61300 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 25 mg/kg

TOXIC EFFECTS :: Vascular - BP lowering not characterized in autonomic section Cardiac - EKG changes not diagnostic of specified effects Cardiac - cardiac output

MUTATION DATA

TYPE OF TEST :: Sister chromatid exchange

TEST SYSTEM :: Rodent - hamster Ovary

DOSE/DURATION :: 10 nmol/L

REFERENCE :: CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut Sts., Philadelphia, PA 19106) V.1- 1941- Volume(issue)/page/year: 41,376,1981