Voreloxin (SNS-595) hydrochloride

製品コードS7518 バッチS751801

印刷

化学情報

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

C18H20ClN5O4S
分子量 437.9 CAS No. 175519-16-1
Solubility (25°C)* 体外 DMSO 20 mg/mL (45.67 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.
* <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 Voreloxin hydrochloride (SNS-595, Vosaroxin) is a potent Topoisomerase II inhibitor with broad-spectrum anti-tumor activity. Phase 2.
in vitro Voreloxin exhibits potent inhibitory effect in topoisomerase II relaxation with IC50 of 3.2 μg /mL without effect on topoisomerase II cleavage. Voreloxin has a cytotoxic activity against human tumor cell lines more potent than that of etoposide. [1] Voreloxin has broad anti-proliferative activity in 15 cell lines, including 4 drug-resistant lines, with IC50 ranging from 0.04 to 1.155 μM. [2]
in vivo Voreloxin (50 mg/kg i.p.) shows potent in vivo antitumor activity mice implanted with P388 leukemia cells. [1] Voreloxin (25 mg/kg i.v.) demonstrates strong tumor growth inhibition in 10 of 11 solid tumor (breast, ovarian, colon, lung, gastric, and melanoma) xenograft models, 2 hematologic tumor xenograft models, 3 multidrug resistant tumor models and 3 murine syngeneic tumor models (Colon 26, Lewis Lung carcinoma, M5076 Ovarian Sarcoma). [2]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 P388 leukemia cells
濃度 ~10 μg/mL
反応時間 72 hours
実験の流れ Cells are put into wells of a 96-well microtiter plate in the amount of 0.1 mL/well, preincubated for 24 h except for P388 cells, and incubated with various concentrations of a test compound in the 5% CO2 incubator at 37 ° for 72 h. After the culturing, 0.02 mL of a MTT solution (5 mg/mL) is put in each well, and the cells are cultured for a further 4 h. The medium is removed by suction, and 0.2 mL of DMSO is put in each well to dissolve the formed formazan. The absorbance is measured by Multiskan Bichromatic. The IC50 is defined as the drug concentration needed to produce a 50% reduction of absorbance relative to the control.
動物実験 動物モデル Mice implanted with P388 leukemia cells.
投薬量 ~50 mg/kg
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/15056007/
  • https://pubmed.ncbi.nlm.nih.gov/18931998/

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：

Topoisomerase II as a Novel Antiviral Target against Panarenaviral Diseases [ Viruses, 2022, 15(1)105] PubMed: 36680145
KEAP1 Mutations Drive Tumorigenesis by Suppressing SOX9 Ubiquitination and Degradation [ Adv Sci (Weinh), 2020, 7(21):2001018] PubMed: 33173725
Combination of ERK2 inhibitor VX-11e and voreloxin synergistically enhances anti-proliferative and pro-apoptotic effects in leukemia cells [ Apoptosis, 2019, 24(11-12):849-861] PubMed: 31482470
Venetoclax Synergistically Enhances the Anti-leukemic Activity of Vosaroxin Against Acute Myeloid Leukemia Cells Ex Vivo. [ Target Oncol, 2019, 14(3):351-364] PubMed: 31115744
Predicting effective pro-apoptotic anti-leukaemic drug combinations using co-operative dynamic BH3 profiling [ PLoS One, 2018, 13(1):e0190682] PubMed: 29298347
Early changes in rpS6 phosphorylation and BH3 profiling predict response to chemotherapy in AML cells. [ PLoS One, 2018, 13(5):e0196805] PubMed: 29723246
TAK-733, a Selective MEK Inhibitor, Enhances Voreloxin-induced Apoptosis in Myeloid Leukemia Cells [ Anticancer Res, 2018, 38(11):6147-6156] PubMed: 30396931

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。