Description

Product Description

10-Hydroxycamptothecin (10-HCPT), CAS 19685-09-7, is a hydroxylated semisynthetic derivative of camptothecin, engineered to improve solubility and enhance bioavailability compared to its parent compound. As a topoisomerase I inhibitor, 10-HCPT plays a crucial role in preclinical studies focused on DNA damage, replication stress, apoptosis induction, and cytotoxicity, serving as a key tool for mechanistic investigations in cancer biology, DNA repair pathways, and drug-resistance modeling.

The compound functions primarily through the stabilization of the DNA-topoisomerase I covalent complex, preventing religation of single-strand DNA breaks during replication. This mechanism triggers replication fork collapse, activation of DNA damage response pathways, checkpoint engagement, and apoptosis. Its solution formulation facilitates precise dosing in both in vitro and in vivo experiments, reducing solubility limitations and allowing for reproducible cytotoxicity and pharmacokinetic studies.

Extensive preclinical investigations demonstrate that 10-HCPT induces S-phase arrest, oxidative stress, mitochondrial depolarization, and caspase-dependent apoptosis. These effects render it invaluable for studying cytotoxicity, combination therapy mechanisms, and resistance phenomena such as topoisomerase I mutations and drug efflux transporter activity. Additionally, the compound is employed in combination with chemotherapeutics, kinase inhibitors, and oxidative stress modulators to evaluate synergistic or antagonistic interactions.

In cellular models, 10-HCPT has been shown to activate ATR/ATM kinases, CHK1/CHK2 phosphorylation, and downstream p53-dependent or independent DNA repair pathways. The precise modulation of cell-cycle checkpoints and DNA repair mechanisms makes 10-HCPT a critical reagent for understanding drug-induced cytotoxicity, replication stress, apoptosis regulation, and cell-cycle dynamics in preclinical research.

10-Hydroxycamptothecin Its high purity, solution-based format, and verified batch consistency enable reproducible results in a variety of experimental settings, including cancer cell lines, primary cells, xenograft models, and pharmacokinetic assays. Researchers can leverage 10-HCPT to investigate mechanisms underlying chemotherapeutic sensitivity, DNA repair efficiency, oxidative stress response, and apoptotic regulation, contributing to the development of novel anticancer strategies in preclinical studies.

Product Specifications

Mechanism of Action

Topoisomerase I Inhibition

10-Hydroxycamptothecin selectively stabilizes the DNA-topoisomerase I covalent complex, preventing religation of single-strand breaks generated during DNA replication. This blockade leads to replication fork stalling, accumulation of DNA damage, and activation of ATR/ATM signaling pathways.

DNA Damage and Replication Stress

• Stabilized DNA-topoisomerase I complexes cause replication fork collapse.

• ATR/ATM kinases are activated, phosphorylating CHK1/CHK2 and engaging p53-dependent and independent DNA repair pathways.

• Accumulated DNA damage facilitates studies of cell-cycle checkpoints, cytotoxicity, and apoptosis induction.

Apoptosis Pathways

• Mitochondrial depolarization triggers cytochrome c release.

• ROS generation contributes to oxidative stress-mediated apoptosis.

• Caspase-3 and -9 activation engages intrinsic apoptotic pathways.

Combination and Resistance Studies

10-HCPT is frequently used in combination assays to evaluate synergistic or antagonistic cytotoxicity with chemotherapeutics, kinase inhibitors, and oxidative stress modulators. It is also applied to investigate drug resistance mechanisms, such as topoisomerase I mutations and efflux transporter-mediated drug resistance.

Side Effects

10-Hydroxycamptothecin Cellular Effects:

• Dose-dependent cytotoxicity

• S-phase arrest and replication fork collapse

• ROS-mediated oxidative stress

Apoptotic Effects:

• Mitochondrial apoptosis

• Caspase-3/-9 activation

• p53-dependent and independent pathways

Laboratory Handling:

• Handle under PPE with fume hood protection

• Strictly for laboratory research; cytotoxic properties require caution

Keywords

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Shipping Guarantee

All 10-Hydroxycamptothecin shipments of 10-Hydroxycamptothecin solution are handled using validated cold-chain logistics to preserve compound integrity. Packages are sealed with secondary protective wrapping and continuous temperature monitoring. Products are shipped via express international couriers with tracking and insurance.

Trade Assurance

We 10-Hydroxycamptothecin ensure product authenticity, verified ≥99% purity, and compliance with analytical standards (HPLC, MS, NMR). Each batch includes a Certificate of Analysis (CoA). Replacement or refund is guaranteed for any deviation from listed specifications.

Payment Support

Flexible global payment options are available: PayPal, major credit cards (Visa, MasterCard, American Express), T/T, USDT, Bitcoin, Ethereum. Transactions are encrypted and verified for confidentiality.

Disclaimer

10-Hydroxycamptothecin is supplied for laboratory research only. Not for human or animal use. Researchers must follow safety guidelines. Supplier assumes no liability for misuse.

References

1. PubChem Database: 10-Hydroxycamptothecin (CID 123619) ↗

2. ChEMBL Database: 10-HCPT Bioactivity Summary (CHEMBL380056)  ↗

3. DrugBank: 10-Hydroxycamptothecin – DB13929 ↗

4. PubMed ID 21725888: Mechanistic studies of 10-Hydroxycamptothecin-induced apoptosis  ↗

5. IUPHAR/BPS Guide to Pharmacology: Topoisomerase Inhibitors ↗