(S)-10-Hydroxycamptothecin

Catalog No.S2423 Batch:S242303

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Technical Data

Formula

C20H16N2O5
Molecular Weight 364.35 CAS No. 19685-09-7
Solubility (25°C)* In vitro DMSO 18 mg/mL (49.4 mM)
Water Insoluble
Ethanol Insoluble
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description (S)-10-Hydroxycamptothecin (10-HCPT) is a DNA topoisomerase I inhibitor with potent anti-tumor activity.
Targets
DNA topoisomerase I [1]
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]

Protocol (from reference)

Cell Assay:[2]
  • Cell lines

    MDA-231, and BT-20 cells

  • Concentrations

    Dissolved in DMSO, final concentrations ~50 μM

  • Incubation Time

    72 hours

  • Method

    Cells are exposed to various concentrations of 10-Hydroxycamptothecin for 72 hours. Cell growth is monitored by the standard MTT assay.
Animal Study:[4]
  • Animal Models

    BALB/c-nu mice transplanted subcutaneously with Colo 205 cells

  • Dosages

    ~7.5 mg/kg

  • Administration

    Orally once per two days

Selleck's (S)-10-Hydroxycamptothecin has been cited by 9 publications

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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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