| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 500mg |
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Pirarubicin hydrochloride (THP), an analogue of anthracycline, is an anti-neoplastic doxorubicin which acts as a topoisomerase II inhibitor, and is used for treatment of various cancers, in particular, solid tumors. It inhibits DNA replication by intercalating into DNA, interacting with Topo II (topoisomerase II). M5076 cells quickly absorb pirarubicin, and its intracellular concentration surpasses that of doxorubicin by a factor of 2.5. When it comes to the 50% concentration in vitro that inhibits cell growth, pirarubicin works better than doxorubicin. In MG-63 cells, pirarubicin increases Bax expression while suppressing the expression of PCNA, cyclin D1, cyclin E, and Bcl-2.
| Targets |
Topoisomerase II
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| ln Vitro |
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| ln Vivo |
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| Cell Assay |
Cell survival analysis is done using MTS. In short, 96-well plates are used to plate cells in triplicate, with 2 × 103 cells per well, and the cells are then cultured in growth medium. Following that, cells are exposed to pirarubicin for 24 hours at three different concentrations: 2.5 μg/mL, 5 μg/mL, and 10 μg/mL. Once added, the MTS reagent (5 mg/mL) is incubated for 4 hours at 37°C. A microplate reader is used to measure the absorbance at 490 nm[3].
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| Animal Protocol |
A single injection into the caudal vein of 18 mg/kg pirarubicin creates an acute cardiac toxicity model. Thirty-six rats are randomized equally into six groups: low-dose rutin (25 mg/kg), middle-dose rutin (50 mg/kg), high-dose rutin (100 mg/kg), cardiac injury (THP) model, and dexrazoxane (180 mg/kg). The rats in the rutin-treated group receive a single injection of 18 mg/kg of pirarubicin via the caudal vein, as well as varying doses of rutin and CMC-Na by gavage for seven days. For six days, rats in the dexrazoxane-treated group are gavaged with sodium carboxymethylcellulose (CMC-Na). On day 7, rats receive an intraperitoneal injection of 40 mg/kg dexrazoxane and a caudal vein injection of 18 mg/kg pirarubicin. Rats in the THP model group are given CMC-Na by gavage for seven days, and on day seven, they are given an injection of pirarubicin (18 mg/kg) into the caudal vein. The normal control group of rats is given CMC-Na by gavage for seven days, and on day seven, they receive an injection of saline into their caudal vein[4].
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| References |
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| Molecular Formula |
C32H38CLNO12
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|---|---|
| Molecular Weight |
664.09663
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| Exact Mass |
663.21
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| Elemental Analysis |
C, 57.88; H, 5.77; Cl, 5.34; N, 2.11; O, 28.91
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| CAS # |
95343-20-7
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| Related CAS # |
Pirarubicin;72496-41-4
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| Appearance |
Solid powder
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| SMILES |
C[C@H]1[C@H]([C@H](C[C@@H](O1)O[C@H]2C[C@@](CC3=C2C(=C4C(=C3O)C(=O)C5=C(C4=O)C(=CC=C5)OC)O)(C(=O)CO)O)N)O[C@@H]6CCCCO6.Cl
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| InChi Key |
ZPHYPKKFSHAVOE-YZIXBPQXSA-N
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| InChi Code |
InChI=1S/C32H37NO12.ClH/c1-14-31(45-21-8-3-4-9-42-21)17(33)10-22(43-14)44-19-12-32(40,20(35)13-34)11-16-24(19)30(39)26-25(28(16)37)27(36)15-6-5-7-18(41-2)23(15)29(26)38;/h5-7,14,17,19,21-22,31,34,37,39-40H,3-4,8-13,33H2,1-2H3;1H/t14-,17-,19-,21+,22-,31+,32-;/m0./s1
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| Chemical Name |
(7S,9S)-7-[(2R,4S,5S,6S)-4-amino-6-methyl-5-[(2R)-oxan-2-yl]oxyoxan-2-yl]oxy-6,9,11-trihydroxy-9-(2-hydroxyacetyl)-4-methoxy-8,10-dihydro-7H-tetracene-5,12-dione;hydrochloride
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| Synonyms |
Pirarubicin HCl; Pirarubicin hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~20.8 mg/mL (~31.4 mM)
H2O: < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.13 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5058 mL | 7.5290 mL | 15.0580 mL | |
| 5 mM | 0.3012 mL | 1.5058 mL | 3.0116 mL | |
| 10 mM | 0.1506 mL | 0.7529 mL | 1.5058 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04437160 | Recruiting | Drug: Epirubicin or Pirarubicin Drug: Cyclophosphamide |
Triple Negative Breast Cancer | Chinese Academy of Medical Sciences |
February 1, 2020 | Phase 2 |
| NCT05287308 | Not yet recruiting | Drug: pirarubicin Drug: cyclophosphamide |
Breast Cancer | Chinese Academy of Medical Sciences |
March 2022 | Not Applicable |
| NCT02613026 | Completed | Drug: Pirarubicin Drug: Docetaxel |
Breast Neoplasms | 307 Hospital of PLA | July 2009 | Phase 3 |
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