(S)-10-Hydroxycamptothecin

製品コードS2423 バッチS242303

印刷

化学情報

Chemical Structure Synonyms 10-HCPT Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20H16N2O5
分子量 364.35 CAS No. 19685-09-7
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 18 mg/mL (49.4 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 40%PEG300 5%Tween80 50%ddH2O
0.3mg/ml Taking the 1 mL working solution as an example, add 50 μL of 6 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
0.1mg/ml Taking the 1 mL working solution as an example, add 50 μL of 2 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 (S)-10-Hydroxycamptothecin (10-HCPT) is a DNA topoisomerase I inhibitor with potent anti-tumor activity.
in vitro 10-Hydroxycamptothecin inhibits the growth of BT-20 and MDA-231 cell with IC50 of 34.3 nM and 7.27 nM, respectively, more potently than camptothecin (CPT) with IC50 of >500 nM. 10-Hydroxycamptothecin potently induces human topoisomerase I-mediated cleavable complex formation of pBR322 plasmid DNA with EC50 of 0.35 μM, displaying >50-fold potency than CPT with EC50 of 18.85 μM. [2] 10-Hydroxycamptothecin treatment induces dose-dependent growth inhibition of human microvascular endothelial cells (HMEC) with IC50 of 0.31 μM, and significantly inhibits the migration of HMEC with IC50 of 0.63 μM. Treatment of HMEC cells with 10-Hydroxycamptothecin also results in a dose-dependent inhibition of tube formation with IC50 of 0.96 μM. [3] 10-Hydroxycamptothecin (5-20 nM) significantly inhibits the proliferation of Colo 205 cells, arrests the cells in the G2 phase of the cell cycle and induces apoptosis through a caspase-3-dependent pathway. [4]
in vivo 10-Hydroxycamptothecin treatment inhibits angiogenesis in a concentration-dependent fashion in the CAM model, with 95% inhibition at dose of 25 nM, more potently than suramin which at 125 nM inhibits angiogenesis only by 60%. [3] Oral administration of 10-Hydroxycamptothecin at low doses of 2.5-7.5 mg/kg every 2 days leads to significant growth inhibition of Colo 205 xenografts in mice without acute toxicity. [4] LD50: Mice 104mg/kg (i.p.). [5]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 MDA-231, and BT-20 cells
濃度 Dissolved in DMSO, final concentrations ~50 μM
反応時間 72 hours
実験の流れ Cells are exposed to various concentrations of 10-Hydroxycamptothecin for 72 hours. Cell growth is monitored by the standard MTT assay.
動物実験 動物モデル BALB/c-nu mice transplanted subcutaneously with Colo 205 cells
投薬量 ~7.5 mg/kg
投与方法 Orally once per two days

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：

Neddylation inhibitor MLN4924 sensitizes head and neck squamous carcinoma cells to (S)-10-hydroxycamptothecin [ Eur J Med Res, 2023, 28(1):326] PubMed: 37689760
Neddylation inhibitor MLN4924 sensitizes head and neck squamous carcinoma cells to (S)-10-hydroxycamptothecin [ Eur J Med Res, 2023, 28(1):326] PubMed: 37689760
Synthetic lethality between TP53 and ENDOD1 [ Nat Commun, 2022, 13(1):2861] PubMed: 35606358
Evaluating the therapeutic efficacy of triptolide and (S)-10-hydroxycamptothecin on cutaneous and ocular Herpes Simplex Virus type-1 infections in mice [ Heliyon, 2022, 8(8):e10348] PubMed: 36090228
Drastic Modulation of Molecular Packing and Intrinsic Dissolution Rates by Meniscus-Guided Coating of Extremely Confined Pharmaceutical Thin Films [ ACS Appl Mater Interfaces, 2021, 13(47):56519-56529] PubMed: 34783517
Implication of Ataxia-Telangiectasia-mutated kinase in epithelium-mesenchyme transition [ Carcinogenesis, 2021, bgab002] PubMed: 33417668
A natural product, (S)-10-Hydroxycamptothecin inhibits pseudorabies virus proliferation through DNA damage dependent antiviral innate immunity [ Vet Microbiol, 2021, 265:109313] PubMed: 34968801
AMPK-mTOR-ULK1 axis activation-dependent autophagy promotes hydroxycamptothecin-induced apoptosis in human bladder cancer cells. [ J Cell Physiol, 2019, 10.1002/jcp.29307] PubMed: 31621074
DW09849, a selective phosphatidylinositol 3-kinase (PI3K) inhibitor, prevents PI3K signaling and preferentially inhibits proliferation of cells containing the oncogenic mutation p110α (H1047R) [Liu JL, et al. J Pharmacol Exp Ther, 2014, 348(3):432-41] PubMed: 24361696

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。