research use only
Cat.No.S2423
| Related Targets | HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis PPAR Sirtuin Casein Kinase eIF |
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| Other Topoisomerase Inhibitors | Camptothecin (CPT) Beta-Lapachone Amonafide Voreloxin (SNS-595) hydrochloride Ellagic acid Genz-644282 Hydroxy Camptothecine Rubitecan Eleutherin Clinafloxacin |
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In vitro |
DMSO
: 18 mg/mL
(49.4 mM)
Water : Insoluble Ethanol : Insoluble |
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In vivo |
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| Molecular Weight | 364.35 | Formula | C20H16N2O5 |
Storage (From the date of receipt) | |
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| CAS No. | 19685-09-7 | Download SDF | Storage of Stock Solutions |
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| Synonyms | 10-HCPT | Smiles | CCC1(C2=C(COC1=O)C(=O)N3CC4=C(C3=C2)N=C5C=CC(=CC5=C4)O)O | ||
| Targets/IC50/Ki |
DNA topoisomerase I
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|---|---|
| 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. 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. 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.
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| 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%. 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. LD50: Mice 104mg/kg (i.p.).
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References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06143774 | Recruiting | Advanced Solid Tumor |
TaiRx Inc. |
October 31 2023 | Phase 1 |
| NCT04209595 | Active not recruiting | Small Cell Lung Cancer|Extra-Pulmonary Small Cell Carcinomas |
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) |
April 8 2020 | Phase 1|Phase 2 |
| NCT01963182 | Completed | First Line Metastatic Colorectal Cancer |
Centre Jean Perrin |
October 2013 | Phase 2 |
| NCT00520390 | Completed | Lymphoma|Advanced Solid Tumors |
Enzon Pharmaceuticals Inc. |
May 2007 | Phase 1 |
| NCT00520637 | Completed | Advanced Solid Tumors|Lymphoma |
Enzon Pharmaceuticals Inc. |
May 2007 | Phase 1 |
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