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95343-20-7

中文名稱 吡柔比星鹽酸鹽
英文名稱 Pirarubicin (Hydrochloride)
CAS 95343-20-7
分子式 C32H37NO12.HCl
分子量 664.1
MOL 文件 95343-20-7.mol
95343-20-7 結(jié)構(gòu)式 95343-20-7 結(jié)構(gòu)式

基本信息

中文別名
吡柔比星鹽酸鹽
英文別名
CS-1183
Pinorubin
NSC 654509
irarubicin
Terarubicin
THP hydrochloride
THP-adriamycin HCl
(7S,9S)-7-[(2R,4S,5S,6S)-4-amino-6-methyl-5-[(2S)-oxan-2-yl]oxyoxan-2-yl]oxy-6,9,11-trihydroxy-9-(2-hydroxyacetyl)-4-methoxy-8,10-dihydro-7H-tetracene-5,12-dione

物理化學(xué)性質(zhì)

儲(chǔ)存條件Inert atmosphere,Room Temperature
溶解度DMSO: 20.83 mg/mL (31.37 mM); Water: < 0.1 mg/mL (insoluble)
形態(tài)Solid
顏色Pink to red

常見問題列表

生物活性
Pirarubicin Hydrochloride (THP Hydrochloride) 是一種蒽環(huán)類抗生素,為拓?fù)洚悩?gòu)酶 II (topoisomerase II) 的抑制劑,可用于各種癌癥尤其是實(shí)體瘤的研究。
靶點(diǎn)

Topoisomerase II

體外研究

Pirarubicin is a topoisomerase II inhibitor. Pirarubicin shows inhibitory activities against M5076 and Ehrlich cells, with IC 50 s of 0.366 and 0.078 μM, respectively. The cytotoxicity of Pirarubicin toward M5076 cells is lower than toward Ehrlich cells, and this is due to the much lower expression of topoisomerase II in M5076 cells than in Ehrlich cells. Pirarubicin (2.5, 5, 10 μg/mL) significantly induces autophagy in a dose dependent manner in bladder cancer (T24, EJ, 5637, J82 and UM-UC-3) cells. Furthmore, Pirarubicin (5 μg/mL) induces apoptosis through inhibition of mTOR/p70S6K/4E-BP1 in bladder cancer cells, and this effect is enhanced by inhibition of autophagy.

體內(nèi)研究

Pirarubicin (18 mg/kg, i.v.) significantly elevates serum level of BNP, CK-MB, CTnT, LDH, and MDA compared with those in the control group in acute cardiac toxicity rats. Pirarubicin also lowers heart rate, and depresses R-wave voltage, and prolongation of QT intervals in the acute cardiac toxicity model.

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