阿霉素是一種來源于細(xì)菌培養(yǎng)物的半合成抗癌劑。[1]它是一種蒽環(huán)類抗生素。它被廣泛用于血癌、實(shí)體瘤和肉瘤。 鹽酸阿霉素嵌入DNA雙鏈并抑制DNA拓?fù)洚悩?gòu)酶II的進(jìn)程，停止復(fù)制過程。[2]鹽酸阿霉素還誘導(dǎo)組蛋白從開放染色質(zhì)中逐出，導(dǎo)致DNA損傷和表觀遺傳失調(diào)。[3]

    鹽酸阿霉素通過靜脈給藥。大約75%的多柔比星及其代謝物與血漿蛋白結(jié)合。鹽酸阿霉素不穿過血腦屏障。主要通過膽汁排泄，50%的藥物從體內(nèi)不變地消除。剩余的經(jīng)歷單電子還原、雙電子還原和去糖苷化。主要代謝物是一種有效的膜離子泵抑制劑，與心肌病有關(guān)。[4]

產(chǎn)品性質(zhì)：

Cas No.:25316-40-9

別名:鹽酸阿霉素; Hydroxydaunorubicin hydrochloride

化學(xué)名: (7S,9S)-7-[(2R,4S,5S,6S)-4-amino-5-hydroxy-6-methyloxan-2-yl]oxy-6,9,11-trihydroxy-9-(2-hydroxyacetyl)-4-methoxy-8,10-dihydro-7H-tetracene-5,12-dione;hydrochloride

Canonical SMILES CC1C(C(CC(O1)OC2CC(CC3=C(C4=C(C(=C23)O)C(=O)C5=C(C4=O)C=CC=C5OC)O)(C(=O)CO)O)N)O.Cl

分子式:C27H29NO11.HCl

分子量:579.98

溶解度:33.3mg/ml in Water(Need ultrasonic);DMSO : >20 mg/mL (34.48 mM; Need ultrasonic)

儲存條件:4°C, protect from light

注意事項(xiàng)：

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References:

[1]Brayfield, A, ed. (2013). Doxorubicin. Martindale: The Complete Drug Reference. Pharmaceutical Press. Retrieved 15 April 2014.

[2]Pommier Y., et al. (2010). DNA topoisomerases and their poisoning by anticancer and antibacterial drugs. Chemistry & Biology 17 (5): 421–433.

[3]Pang, B., et al. (2013). Drug-induced histone eviction from open chromatin contributes to the chemotherapeutic effects of doxorubicin. Nature Communications 4 (5): 1908

[4]Boucek RJ., et al. (1987). The major metabolite of doxorubicin is a potent inhibitor of membrane-associated ion pumps. A correlative study of cardiac muscle with isolated membrane fractions. J of Biol Chem 262: 15851-15856.