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Pirarubicin Hydrochloride Sale

(Synonyms: 盐酸吡柔比星; THP Hydrochloride) 目录号 : GC36928

An anthracycline antitumor antibiotic

Pirarubicin Hydrochloride Chemical Structure

Cas No.:95343-20-7

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10mM (in 1mL DMSO)
¥544.00
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10mg
¥495.00
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50mg
¥1,890.00
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100mg
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Cell experiment:

MTS is used to analyze cell survival. Briefly, cells are plated in 96-well plates in triplicate at 2 × 103 cells per well and cultured in growth medium. Then cells are treated with pirarubicin at different concentrations (2.5 μg/mL, 5 μg/mL, 10 μg/mL) for 24 h. MTS reagent (5 mg/mL) is added and incubated at 37°C for 4 h. The absorbance is monitored at 490 nm using a microplate reader[3].

Animal experiment:

An acute cardiac toxicity model is established by a single dose of 18 mg/kg pirarubicin through the caudal vein injection. Thirty-six rats are randomized equally to six groups: normal control, cardiac injury (THP) model, dexrazoxane (180 mg/kg), low-dose rutin (25 mg/kg), middle-dose rutin (50 mg/kg), and high-dose rutin (100 mg/kg). Rats in the rutin-treated group are administered different doses of rutin and CMC-Na for 7 days by gavage and a single dose of 18 mg/kg pirarubicin through caudal vein injection. Rats in the dexrazoxane-treated group receive sodium carboxymethylcellulose (CMC-Na) by gavage for six days. 40 mg/kg dexrazoxane is then administered to rats by intraperitoneal injection and 18 mg/kg pirarubicin is administered by caudal vein injection on day 7. Rats in the THP model group receive CMC-Na by gavage for seven days, followed by pirarubicin 18 mg/kg through the caudal vein injection on day 7. Rats in the normal control group receive CMC-Na by gavage for seven days, followed by saline through caudal vein injection on day 7[4].

References:

[1]. Takigawa N, et al. Cytotoxic effect of topoisomerase II inhibitors against adriamycin- and etoposide-resistant small cell lung cancer sublines. Gan To Kagaku Ryoho. 1993 May;20(7):929-35.
[2]. Nagai K, et al. Relationships between the in vitro cytotoxicity and transport characteristics of pirarubicin and doxorubicin in M5076 ovarian sarcoma cells, and comparison with those in Ehrlich ascites carcinoma cells. Cancer Chemother Pharmacol. 2002 Mar;49(3):244-50. Epub 2002 Jan 8.
[3]. Li K, et al. Pirarubicin induces an autophagic cytoprotective response through suppression of the mammalian target of rapamycin signaling pathway in human bladder cancer cells. Biochem Biophys Res Commun. 2015 May 1;460(2):380-5.
[4]. Wang YD, et al. Cardioprotective effects of rutin in rats exposed to pirarubicin toxicity. J Asian Nat Prod Res. 2017 Oct 27:1-13.

产品描述

Pirarubicin is an anthracycline that has anticancer activity.1 It interacts with topoisomerase II to inhibit DNA replication. Pirarubicin inhibits the growth of human HeLa and C33A cervical, as well as T-24 bladder cancer cells (IC50s = 29, 52, and 36 ng/ml, respectively).2 It inhibits the growth of human Huh7 and MHCC97H liver cancer cells (IC50s = 0.159 and 0.374 μM, respectively).3 Pirarubicin also inhibits the growth of M5076 mouse ovarian cancer cells in vitro (IC50 = 0.366 μM) and in vivo in a mouse allograft model when administered at a dose of 2 mg/kg for four days.4

1.Monneret, C.Recent developments in the field of antitumour anthracyclinesEur. J. Med. Chem.36(6)483-493(2001) 2.Tsuchiya, K.S., Ishii, T., Ikeno, S., et al.Inhibition of anchorage-independent growth of tumor cells by IT-62-B, a new anthracyclineJ. Antibiot. (Tokyo)50(10)853-859(1997) 3.Huang, H., Chen, T., Zhou, Y., et al.RIPK1 inhibition enhances pirarubicin cytotoxic efficacy through AKT-P21-dependent pathway in hepatocellular carcinomaInt. J. Med. Sci.15(14)1648-1657(2018) 4.Sugiyama, T., Sadzuka, Y., Nagasawa, K., et al.Membrane transport and antitumor activity of pirarubicin, and comparison with those of doxorubicinJpn. J. Cancer Res.90(7)775-780(1999)

Chemical Properties

Cas No. 95343-20-7 SDF
别名 盐酸吡柔比星; THP Hydrochloride
Canonical SMILES O=C1C2=C(C=CC=C2OC)C(C3=C(O)C4=C([C@@H](O[C@@]5([H])C[C@H](N)[C@H](O[C@@]6([H])OCCCC6)[C@H](C)O5)C[C@@](C(CO)=O)(O)C4)C(O)=C31)=O.Cl
分子式 C32H38ClNO12 分子量 664.1
溶解度 DMSO: 20.83 mg/mL (31.37 mM); Water: < 0.1 mg/mL (insoluble) 储存条件 4°C, protect from light
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1 mM 1.5058 mL 7.529 mL 15.058 mL
5 mM 0.3012 mL 1.5058 mL 3.0116 mL
10 mM 0.1506 mL 0.7529 mL 1.5058 mL
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Research Update

Anaphylactic shock due to intravesical administration of Pirarubicin Hydrochloride for the fifth time

J Clin Anesth 2016 Feb;28:2-3.PMID:26796606DOI:10.1016/j.jclinane.2015.08.001.

We report the first case of anaphylaxis induced by intravesical administration of Pirarubicin Hydrochloride during spinal anesthesia. The patient was a 64-year-old woman being followed up for transitional cell carcinoma of the bladder. Anaphylaxis occurred the fifth time Pirarubicin Hydrochloride was administered intravesically. Pirarubicin Hydrochloride, an anthracycline antitumor antibiotic that is widely used for intravesical instillation chemotherapy, is administered at the end of surgery. Because this is about the time that the patient is leaving the operating room, attention to patient monitoring tends to be divided. Because anaphylaxis may occur at this time, staff should remain vigilant of the risk of anaphylaxis.