Topotecan

製品コードS9321 バッチS932106

印刷

化学情報

Chemical Structure Synonyms NSC609699,Nogitecan,SKFS 104864A Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C23H23N3O5
分子量 421.45 CAS No. 123948-87-8
Solubility (25°C)* 体外 DMSO 84 mg/mL (199.31 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）
Clear solution
5% DMSO 95% Corn oil
0.15mg/ml Taking the 1 mL working solution as an example, add 50 μL of 3 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. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
2.1mg/ml Taking the 1 mL working solution as an example, add 50 μL of 42 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. 
* <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 Topotecan(NSC609699,Nogitecan,SKFS 104864A) is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases.
in vitro

Topotecan exhibits inhibition of outgrowth of the highly invasive and migratory leader cells (LC) population, however, topotecan enrichs the LC subset 20% above the untreated control level.[2]
in vivo

Topotecan (TPT), at least in part by inhibiting expression of Fli-1, significantly ameliorates lupus nephritis in NZBWF1 mice as effectively or better than cyclophosphamide (CYC).[3]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 LC-T2A-GFP lines
濃度 1 μM
反応時間 72 h
実験の流れ

LC-T2A-GFP lines are seeded at 1200 cells per well of a 384-well plate, adhered overnight, and treated with chemotherapeutics olaparib, rucaparib, paclitaxel, topotecan, carboplatin, cyclophosphamide, cisplatin, and doxorubicin at empirically determined clinically relevant doses (1 μM). Cells are maintained at 37 ℃ with 5% CO2 in treatment for 72 h. Four focal areas per replicate well were imaged using 4X magnification on a bright field.
動物実験 動物モデル NZBWF1 female mice
投薬量 0.03 mg/kg, 0.1 mg/kg, 0.3mg/kg
投与方法 i.p.

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：

Identification and targeting of protein tyrosine kinase 7 (PTK7) as an immunotherapy candidate for neuroblastoma [ Cell Rep Med, 2023, 4(6):101091] PubMed: 37343516
Immune suppressive signaling regulated by latent transforming growth factor beta binding protein 1 promotes metastasis in cervical cancer [ Braz J Med Biol Res, 2023, 55:e12206] PubMed: 36629522
FL118, acting as a 'molecular glue degrader', binds to dephosphorylates and degrades the oncoprotein DDX5 (p68) to control c-Myc, survivin and mutant Kras against colorectal and pancreatic cancer with high efficacy [ Clin Transl Med, 2022, 12(5):e881] PubMed: 35604033
Secreted HSP90α-LRP1 Signaling Promotes Tumor Metastasis and Chemoresistance in Pancreatic Cancer [ Int J Mol Sci, 2022, 23(10)5532] PubMed: 35628341
Adamantane-Monoterpenoid Conjugates Linked via Heterocyclic Linkers Enhance the Cytotoxic Effect of Topotecan [ Molecules, 2022, 27(11)3374] PubMed: 35684313
Immunogenicity of small-cell lung cancer associates with STING pathway activation and is enhanced by ATR and TOP1 inhibition [ Cancer Med, 2022, 10.1002/cam4.5109] PubMed: 35957613
SMARCA4/2 loss inhibits chemotherapy-induced apoptosis by restricting IP3R3-mediated Ca2+ flux to mitochondria [ Nat Commun, 2021, 12(1):5404] PubMed: 34518526
Camptothecin and topotecan, inhibitors of transcription factor Fli-1 and topoisomerase, markedly ameliorate lupus nephritis in NZBWF1 mice and reduce the production of inflammatory mediators in human renal cells [ Arthritis Rheumatol, 2021, 10.1002/art.41685] PubMed: 33559345
Chemoresistance is mediated by ovarian cancer leader cells in vitro [ J Exp Clin Cancer Res, 2021, 40(1):276] PubMed: 34470672
FK228 potentiates topotecan activity against small cell lung cancer cells via induction of SLFN11 [ Acta Pharmacol Sin, 2021, 10.1038/s41401-021-00817-y] PubMed: 34893686

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。