Pirarubicin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Pirarubicin 是一种蒽环类抗生素，也是一种 DNA/RNA 合成抑制剂，通过插入 DNA 并与拓扑异构酶 II 相互作用，用作抗肿瘤剂。

Pirarubicin is an anthracycline antibiotic, and also a DNA/RNA synthesis inhibitor by intercalating into Dna and interacts with topoisomerase II, used as an antineoplastic agent.(In Vitro):Pirarubicin is a topoisomerase II inhibitor. Pirarubicin shows inhibitory activities against M5076 and Ehrlich cells, with IC50s 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.(In Vivo):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.

Pirarubicin is a topoisomerase II inhibitor. Pirarubicin shows inhibitory activities against M5076 and Ehrlich cells, with IC50s 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.

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.

Tepirubicin | Tetrahydropyranyl-Doxorubicin | THP-Adriamycin | THP-Doxorubicin

Cell Cycle/DNA Damage

Topoisomerase

Topo II

Cancer

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72496-41-4

627.64

C32H37NO12

>98% (HPLC)

DMSO:7 mg/mL (11.15 mM); Ethanol:<1 mg/mL (<1 mM); Water:<1 mg/mL (<1 mM)

O=C1C2=C(O)C(C[C@](C(CO)=O)(O)C[C@@H]3O[C@H]4C[C@H](N)[C@H](O[C@H]5CCCCO5)[C@H](C)O4)=C3C(O)=C2C(C6=C1C=CC=C6OC)=O

(8S,10S)-10-(((2R,4S,5S,6S)-4-amino-6-methyl-5-(((S)-tetrahydro-2H-pyran-2-yl)oxy)tetrahydro-2H-pyran-2-yl)oxy)-6,8,11-trihydroxy-8-(2-hydroxyacetyl)-1-methoxy-7,8,9,10-tetrahydrotetracene-5,12-dione

(-20℃)

With Ice Pack

≥ 2 years