Pirarubicin

製品コードS1393 バッチS139308

印刷

化学情報

Chemical Structure Synonyms NSC-333054,THP Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C32H37NO12
分子量 627.64 CAS No. 72496-41-4
Solubility (25°C)* 体外 DMSO 100 mg/mL (159.32 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 1.650mg/ml (2.63mM) Taking the 1 mL working solution as an example, add 50 μL of 33 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 0.830mg/ml (1.32mM) Taking the 1 mL working solution as an example, add 50 μL of 16.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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 rapidly taken up by M5076 cells and the intracellular concentration of this compound reaches more than 2.5-fold that of doxorubicin. It is more effective than doxorubicin in terms of the 50% cell growth-inhibitory concentration in vitro. [1] This compound causes G0/G1 cell cycle arrest in MG-63 cells. It suppresses the expression of PCNA, cyclin D1, cyclin E and Bcl-2, and increases Bax expression in MG-63 cells. [2] This agent markedly relaxes contractions induced by noradrenaline (0.1 μM) in the aorta with endothelium, but not in that without endothelium. The relaxation induced by this chemical is inhibited by methylene blue (5 μM), hydroquinone (100 μM), phenidone (50 μM), haemoglobin (1 μM) and p-bromophenacyl bromide (50 μM), but not by indomethacin (25 μM). [3] It is approximately 2-5 times more potent than Adriamycin in SKUT1B, HEC1A, and BG1 cell lines. This compound also displays a reverse dose-response pattern of G2 block so that at high dose, cell cycle kinetics would mirror those of untreated controls. [4]
in vivo

Pirarubicin reduces the tumor weight to 60% of the control level in M5076 solid tumor-bearing mice, although doxorubicin has no effect. [1] This compound and Epirubicin are effective against V x 2 tumor when injected via the hepatic intra-arterial (h.i.a.) route, the activity of this chemical is stronger than that of Epirubicin. [5]

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/10470291/
  • https://pubmed.ncbi.nlm.nih.gov/20357441/
  • https://pubmed.ncbi.nlm.nih.gov/1687584/
  • https://pubmed.ncbi.nlm.nih.gov/1592283/
  • https://pubmed.ncbi.nlm.nih.gov/7880733/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Wnt signaling modulates the response to DNA damage in the Drosophila wing imaginal disc by regulating the EGFR pathway [ PLoS Biol, 2024, 22(7):e3002547] PubMed: 39047051
Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862] PubMed: 39319271
Patient-derived organoid culture of gastric cancer for disease modeling and drug sensitivity testing [ Biomed Pharmacother, 2023, 163:114751] PubMed: 37105073
Nkx2.8 promotes chemosensitivity in bladder urothelial carcinoma via transcriptional repression of MDR1 [ Cell Death Dis, 2022, 13(5):492] PubMed: 35610207
Lipoparticles for Synergistic Chemo-Photodynamic Therapy to Ovarian Carcinoma Cells: In vitro and in vivo Assessments [ Int J Nanomedicine, 2021, 16:951-976] PubMed: 33603362
Synthesis and In Vitro Assessment of pH-Sensitive Human Serum Albumin Conjugates of Pirarubicin [ Pharmaceuticals (Basel), 2020, 14(1)E22] PubMed: 33396604
Gene Essentiality Profiling Reveals Gene Networks and Synthetic Lethal Interactions with Oncogenic Ras. [ Cell, 2019, 36(2):179-193] PubMed: 28162770
A Pharmacogenomic Landscape in Human Liver Cancers. [ Cancer Cell, 2019, 36(2):179-193] PubMed: 31378681
Dual Inhibition of Pirarubicin-Induced AKT and ERK Activations by Phenformin Sensitively Suppresses Bladder Cancer Growth. [ Front Pharmacol, 2019, 10:1159] PubMed: 31649535
MARCH1 encourages tumour progression of hepatocellular carcinoma via regulation of PI3K-AKT-β-catenin pathways. [ J Cell Mol Med, 2019, 23(5):3386-3401] PubMed: 30793486

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。