盐酸阿柔比星

生物活性靶点体外研究体内研究盐酸阿柔比星试剂级价格

盐酸阿柔比星

CAS号:75443-99-1
英文名:ACLARUBICIN HYDROCHLORIDE
中文名:盐酸阿柔比星
CBNumber:CB2189954
分子式:C42H54ClNO15
分子量:848.33
MOL File:75443-99-1.mol

盐酸阿柔比星化学性质

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

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

盐酸阿柔比星化学药品说明书

注射用盐酸阿柔比星

盐酸阿柔比星性质、用途与生产工艺

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.