中文名称:

盐酸阿柔比星

中文同义词:

盐酸阿柔比星;阿柔比星盐酸盐

英文名称:

ACLARUBICIN HYDROCHLORIDE

英文同义词:

aclacinomycinahydrochloride;aclacinon;n-2-yl)-alpha-l-lyxo-hexopyranosyl)-3-(dimethylamino)-alpha-l-lyxo-hexopyrano;syl)oxy)-2,5,7-trihydroxy-,methylester,hydrochloride,(1r-(1-alpha,2-beta,4;1-Naphthacenecarboxylic acid, 2-ethyl-1,2,3,4,6,11-hexahydro-2,5,7-trihydroxy-6,11-dioxo-4-[[2,3,6-trideoxy-4-O-[2,6-dideoxy-4-O-[(2R-trans)-tetrahydro-6-methyl-5-oxo-2H-pyran-2-yl]-alpha-l-lyxo-hexopyranosyl]-3-(dimethylamino)-alpha-l-lyxo;ACLARUBICIN HYDROCHLORIDE;1-Naphthacenecarboxylic acid, 2-ethyl-1,2,3,4,6,11-hexahydro-2,5,7-trihydroxy-6,11-dioxo-4-[[2,3,6-trideoxy-4-O-[2,6-dideoxy-4-O-[(2R,6S)-tetrahydro-6-methyl-5-oxo-2H-pyran-2-yl]-α-L-lyxo-hexopyranosyl]-3-(dimethylamino)-α-L-lyxo-hexopyranosyl]oxy]-, meth;1-Naphthacenecarboxylic acid, 2-ethyl-1,2,3,4,6,11-hexahydro-2,5,7-trihydroxy-6,11-dioxo-4-[[2,3,6-trideoxy-4-O-[2,6-dideoxy-4-O-[(2R-trans)-tetrahydro-6-methyl-5-oxo-2H-pyran-2-yl]-α-L-lyxo-hexopyranosyl]-3-(dimethylamino)-α-L-lyxo-hexopyranosyl]oxy]-, methyl ester, hydrochloride, [1R-(1α,2β,4β)]-

CAS号:

75443-99-1

分子式:

C42H54ClNO15

分子量:

848.33

EINECS号:

278-209-3

相关类别:

API

Mol文件:

75443-99-1.mol

熔点 

151-153℃

沸点 

898℃

闪点 

>110°(230°F)

储存条件 

2-8°C

溶解度 

Soluble in DMSO or DMF at 25mg/ml

生物活性

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。

靶点

20S proteasome. Topoisomerase I and II.

体外研究

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 .

体内研究

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.

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.

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

HazardClass 

6.1(a)

PackingGroup 

II