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盐酸阿柔比星
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CAS号:75443-99-1 | 英文名称:ACLARUBICIN HYDROCHLORIDE
分子式 C42H54ClNO15
分子量 848
EINECS号 278-209-3
MDL MFCD00133024
Smiles
InChIKey
乙二醇化学百科
基本信息
中文名称 盐酸阿柔比星
英文名称 ACLARUBICIN HYDROCHLORIDE
CAS号 75443-99-1
分子式 C42H54ClNO15
分子量 848.33
EINECS号 278-209-3
物化性质
熔点 151-153℃
沸点 898℃
闪点 >110°(230°F)
溶解度 溶于DMSO或DMF,浓度为25mg/ml
形态 固体
颜色 浅黄至黄色
安全信息
危险品标志 T
危险类别码 23/24/25
安全说明 36/37/39-45
危险品运输编号 3249
RTECS号 QI9283500
危险等级 6.1(a)
包装类别 II
生产及用途
Aclacinomycin A hydrochloride (Aclarubicin hydrochloride) 是一种荧光分子,是第一个发现对 20S 蛋白酶体 (20S proteasome) 的 CTRL (糜凝乳蛋白酶样) 活性具有离散特异性的非肽性抑制剂。同时也是 拓扑异构酶 I 和 II (topoisomerase I and II) 的双抑制剂。是一种有效蒽环类化疗试剂用于血癌和实体肿瘤的相关研究。

20S proteasome.
Topoisomerase I and II.

Aclacinomycin A could efficiently enter living cells and emit fluorescence in situ . Aclacinomycin A (10 μM for 15 min) is sufficient for clear detection of fluorescence in most of the cultured cells. Aclacinomycin A treatment (10 μM Acla for 15 min) results in approximately 20% dead (or nearly dead) cells.
Aclacinomycin A (Aclarubicin) effectively induces incorporation of exon 7 into SMN2 transcripts from the endogenous gene in type I SMA fibroblasts as well as into transcripts from a SMN2 minigene in the motor neuron cell line NSC34 .

Aclacinomycin A is very well absorbed in mice, rats, and dogs after its oral administration. The oral LD 50 (76.5 mg/kg) is about twice the iv LD 50 (35.6 mg/kg) in mice [4 .
Aclacinomycin A (0.75-6 mg/kg, ip daily) dose-dependently exhibits tumor growth in mice-based Leukemia P-388 model [4 .

Animal Model: DBA/2, CDF 1 (BALB/c×DBA/2) mice with Leukemia P-388 [4 .
Dosage: 0.75 mg/kg, 1.5 mg/kg, 3 mg/kg, 6 mg/kg.
Administration: Intraperitoneal administration daily for 10 days starting 3 hr after transplantation.
Result: Inhibited tumor growth.
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