カンプトテシン
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カンプトテシン

Camptothecin supplier bulk factory Wholesale buy Extract factory

  1. 英語名: Camptothecin
  1. 仕様
    • 純度: Camptothecin ≥ 98% (HPLC); High – purity grade: ≥ 99% (HPLC)
    • 溶解度: Sparingly soluble in water (approx. 0.1 mg/mL at 25°C), soluble in DMSO, NMP (N – Methyl – 2 – pyrrolidone) and alkaline solutions. Water – soluble derivatives (e.g., sodium salt) have improved solubility.
    • 融点: 260 – 264°C (decomposes)
    • 残留溶媒: DMSO ≤ 0.5%, NMP ≤ 0.5%
    • 重金属: ≤ 10 ppm
    • 粒子サイズ: Standard powder ≤ 100 μm; micronized powder ≤ 5 μm for enhanced bioavailability in formulations
  1. 外観
    • Pale yellow to yellowish – green crystalline powder, odorless
  1. CAS番号：7689 – 03 – 4
  1. リードタイム: 7～10営業日
  1. パッケージ
    • 100 mg/vial (sterile glass vial), 1 g/aluminum foil – lined bag; stored under nitrogen to prevent oxidation
  1. メインマーケット: Global pharmaceutical and research markets, with significant demand in North America, Europe, and Asia, especially in oncology research and drug development
  1. アプリケーションシナリオ

コアプロパティ

  • 分子式: C₂₀H₁₆N₂O₄
  • 化学構造: A pentacyclic quinoline alkaloid, featuring a unique camptothecin ring system with a lactone moiety, which is crucial for its biological activity.
  • 主な特徴
    • Topoisomerase Inhibitor: Specifically targets DNA topoisomerase I, preventing the religation of DNA strands during replication, leading to DNA damage and cell death in rapidly dividing cells.
    • 抗腫瘍活性: Potent cytotoxic effects against a wide range of cancer cell lines, including colorectal, lung, ovarian, and pancreatic cancers.
    • pH – Dependent Stability: The lactone ring is stable in acidic conditions (pH < 4.5) but undergoes hydrolysis to the carboxylate form in neutral and basic environments, reducing its biological activity.
    • High Potency: Low therapeutic doses are required due to its strong inhibitory effect on DNA replication, but this also necessitates careful handling to manage potential toxicity.

アプリケーションシナリオ

1. 腫瘍学研究

  • Pre – clinical Studies:
    • Widely used in in – vitro cell culture experiments and in – vivo animal models to study the mechanism of action of topoisomerase I inhibitors, screen for new anticancer drugs, and evaluate the efficacy of combination therapies.
  • 医薬品開発:
    • Serves as a lead compound for the development of second – generation and third – generation camptothecin – based drugs. Many clinically used anticancer drugs, such as irinotecan and topotecan, are synthetic derivatives of camptothecin with improved solubility, stability, and reduced toxicity.

2. 製薬業界

  • Anticancer Drug Synthesis:
    • As an intermediate in the production of camptothecin – derived drugs. Chemical modifications are made to the camptothecin structure to enhance its pharmacological properties, such as increasing water solubility, stabilizing the lactone ring, and improving targeting ability.
  • 品質管理:
    • Used as a reference standard for the analysis and quality control of camptothecin – based drugs, ensuring the consistency and purity of pharmaceutical products.

3. 生物医学研究

  • DNA Replication and Repair Studies:
    • Helps researchers understand the processes of DNA replication, repair, and the role of topoisomerases in maintaining genomic stability. By inhibiting topoisomerase I, scientists can study the cellular responses to DNA damage and the activation of various repair pathways.
  • Drug Resistance Research:
    • Investigated to understand the mechanisms of drug resistance in cancer cells towards camptothecin and its derivatives. This knowledge can guide the development of strategies to overcome resistance and improve treatment outcomes.

検出方法

  • 高速液体クロマトグラフィー（HPLC）:
    • Column: C18 (250 × 4.6 mm, 5 μm), Mobile Phase: Acetonitrile – 0.1% formic acid (gradient elution), Flow Rate: 1.0 mL/min, Detection Wavelength: 254 nm for quantification.
  • Ultra – Performance Liquid Chromatography – Mass Spectrometry (UPLC – MS):
    • Used for the identification and quantification of camptothecin and its metabolites in biological samples. It provides high – sensitivity and high – resolution analysis, crucial for pharmacokinetic and pharmacodynamic studies.
  • フーリエ変換赤外分光法（FTIR）:
    • Helps in confirming the chemical structure of camptothecin by analyzing the characteristic absorption peaks of its functional groups, ensuring the integrity of the compound during production and storage.

出典と利点

  • 天然源: Originally isolated from the bark and wood of the Chinese tree Camptotheca acuminata. However, due to the low content of camptothecin in the plant (0.01 – 0.03%) and environmental concerns, semi – synthesis and total synthesis methods are now commonly used.
  • 治療の可能性: Its unique mechanism of action makes it a valuable starting point for the development of highly effective anticancer drugs, contributing significantly to the field of oncology.
  • Research Utility: A crucial tool in biomedical research, enabling a deeper understanding of fundamental biological processes related to DNA metabolism and cancer biology.

規制コンプライアンス

  • 米国FDA: Regulated as an investigational new drug (IND) for research purposes and as a pharmaceutical ingredient for approved camptothecin – based drugs. Stringent regulations govern its use in clinical trials and commercial production to ensure patient safety.
  • EU規制: Subject to strict regulations under the European Medicines Agency (EMA). Clinical trials involving camptothecin and its derivatives must comply with Good Clinical Practice (GCP) guidelines, and marketing authorization is required for commercial use.
  • 中国NMPA: Monitored closely in China, especially for drugs derived from camptothecin. The extraction, synthesis, and clinical application of camptothecin – related products need to meet national pharmaceutical standards and regulatory requirements.
カテゴリ： ,

Camptothecin: Nature’s Potent Topoisomerase Inhibitor for Oncology & Analysis | Supplier & Manufacturer

1. What is Camptothecin?

Camptothecin (CPT) is a pentacyclic quinoline alkaloid initially remoted from the bark/stems of the Chinese language Comfortable Tree (Camptotheca acuminata). It features as a potent topoisomerase I (Topo I) inhibitor, binding to the Topo I-DNA advanced and stopping DNA religation throughout replication. This triggers replication fork collapse, double-strand DNA breaks、 そして S-phase selective apoptosis in quickly dividing cells. Its distinctive mechanism underpins its significance in oncology therapeutics そして most cancers biology analysis.

2. 供給、化学的性質および識別子

  • 供給： 主に抽出された Camptotheca acuminata bark/seeds. Semi-synthesis from plant precursors is widespread.

  • 化学的性質:

    • 化学名: (S)-4-Ethyl-4-hydroxy-1H-pyrano[3′,4′:6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione

    • 分子成分: C₂₀H₁₆N₂O₄

    • 分子量: 348.36 g/mol

    • 外観： Pale yellow to gentle inexperienced crystalline powder

    • 溶解度: Lactone ring pH-dependence – Soluble in DMSO, DMF, chloroform (closed lactone kind, energetic); hydrolyzes to inactive carboxylate kind in aqueous pH >7.

    • 安定性： Mild and pH-sensitive. Requires strict management of lactone ring integrity for bioactivity.

  • キー識別子:

    • CAS: 7689-03-4

    • EC数量（EINECS）： 231-684-4

    • MF: C₂₀H₁₆N₂O₄

    • MW: 348.36

3. Purity, Efficacy, Security & Dosage

  • Optimum Product: The “finest” camptothecin options >99% HPLC purity, >95% lactone kind content material (important for exercise), and undetectable contaminants. Shaanxi Zhonghong achieves this by way of proprietary pH-controlled crystallization そして 凍結乾燥.

  • Well being Benefits & Functions:

    • Anticancer Exercise: Core mechanism: Topo I inhibition → DNA harm → S-phase apoptosis. Foundation for FDA-approved derivatives (Irinotecan, Topotecan) treating colorectal, ovarian, SCLC, cervical cancers.

    • Antiviral/Antiparasitic Analysis: Rising exercise towards HIV-1, HSV, Leishmania in preclinical fashions.

    • (Be aware: Nattokinase primarily exhibits anticoagulant/thrombolytic results; direct kidney advantages are much less established vs. potential CPT nephrotoxicity issues).

  • Dosage & Administration:

    • NOT a dietary complement. Used clinically as IV derivatives below strict medical supervision.

    • Analysis doses differ (usually 0.1-100 µM 試験管内; mg/kg ranges 生体内). No secure each day consumption for self-administration exists.

  • Important Precautions & Aspect Results:

    • Extreme Toxicity: Myelosuppression (neutropenia, thrombocytopenia), extreme diarrhea (cholinergic & delayed), hemorrhagic cystitis, hepatotoxicity.

    • Lactone Instability: Speedy hydrolysis to inactive carboxylate at physiological pH reduces efficacy.

    • 禁忌: Being pregnant/lactation (teratogenic), pre-existing bone marrow melancholy, energetic infections.

    • 対処: Cytotoxic – Requires PPE (gloves, masks, lab coat). Keep away from inhalation/pores and skin contact.

4. Shaanxi Zhonghong: Your Premier Camptothecin Supply

Shaanxi Zhonghong Investment Technology Co., Ltd. is a cGMP/ISO-certified chief in high-purity plant-derived APIs. With 28+ years in bioactive phytochemistry, we focus on:

  • Core Capabilities:

    • 科学的卓越性: 5 College Joint Labs, 20+ Patents (incl. CPT stabilization tech), Unique Natural Compound Library.

    • Slicing-Edge Analytics: HPLC-PDA/ELSD (purity), UPLC-QTOF-MS (impurity profiling), Superconducting FT-NMR (construction ID), ICP-MS (heavy metals), GC-MS/MS (residual solvents). Purity >99%, exceeding USP by 20%.

    • 国際的な達成: 提供する 80か国以上 – Pharma, Biotech, Tutorial Analysis.

    • 垂直統合： 持続可能な調達 → GMP Extraction → pH-Managed Purification → 凍結乾燥.

5. Rigorous Product Specs

汚染物質クラス パラメータ 仕様制限 テクニックを見てみよう
農薬 クロルピリホス ≤ 0.01 mg/kg GC-MS/MS
シペルメトリン ≤ 0.05 mg/kg GC-ECD
全く異なる農薬 ≤ 0.1 mg/kg（毎） EU 2021/601
重金属 鉛 ≤ 1.0 mg/kg ICP-MS（USP <232>）
として ≤ 0.5 mg/kg ICP-MS（USP <232>）
CD ≤ 0.5 mg/kg ICP-MS（USP <232>）
水銀 ≤ 0.1 mg/kg CVAAS (USP <232>)
微生物学的 TAMC ≤ 10³ CFU/g USP <61>
TYMC ≤ 10² CFU/g USP <61>
大腸菌 10gには含まれない USP <62>
サルモネラ 属 Absent in 375g USP <62>
Important High quality Camptothecin Purity ≥ 99.0% (HPLC) HPLC-PDA（USP <621>）
Lactone Kind ≥ 95.0% pH-Particular HPLC
水分含有量 ≤ 2.0% Karl Fischer (USP <921>)
残留溶媒 Class 1/2 Solvents: Undetected GC-FID（ICH Q3C）

6. 優れた製造ワークフロー

  1. Sustainable Harvesting: Camptotheca acuminata cultivated below GACP tips.

  2. 選択的抽出： Ethanol/Water または 超臨界CO₂ extraction of bark/seeds.

  3. 主要な浄化： Liquid-liquid partitioning (CH₂Cl₂/H₂O), adsorbent chromatography (SiO₂, polyamide).

  4. Lactone Stabilization: pH-controlled crystallization (pH 3.5-4.5) to maximise lactone yield.

  5. Last Purification: 分取HPLC (C18 column, MeOH/H₂O/TFA cell section).

  6. 乾燥： 凍結乾燥 (-50°C, <10 Pa) to protect lactone ring & stability.

  7. QCの起動: 満杯 CoA verifying identification, purity, lactone content material, contaminants.

7. Key Application Areas

  • Oncology Medicine: Precursor for Irinotecan (CPT-11), Topotecan, Belotecan.

  • Most cancers Analysis: Software compound for DNA harm response, アポトーシス, drug resistance research.

  • Drug Supply Techniques: Loaded into liposomes, nanoparticles, polymer conjugates to boost solubility/concentrating on.

  • Antiviral/Antiparasitic Improvement: Investigational agent for novel therapeutics.

8. cGMP High quality Management Protocol
陝西中宏は tiered QC technique:

  • 識別： FT-NMR (¹H/¹³C), HPLC-UV/PDA spectral match vs. USP reference customary.

  • Assay & Impurities: HPLC-ELSD/PDA quantifies CPT (≥99.0%) and detects ≤0.1% associated compounds (10-deacetylcamptothecin, camptothecin carboxylate).

  • Lactone Content: Validated pH-specific RP-HPLC methodology distinguishes lactone/carboxylate types.

  • 汚染物質: ICP-MS for heavy metals (USP <232>), GC-MS/MS for 500+ pesticides (EU 2021/601), LC-MS/MS for mycotoxins, USP <61>/<62> for microbiology.

  • 安定性： Actual-time & accelerated ICH Q1A(R2) research verify 24-month shelf-life at -20°C (desiccated, argon ambiance).

9. Safe Packaging & Logistics

  • Major Pack: Amber glass vials sealed below argon, full of desiccant.

  • Secondary Pack: Vacuum-sealed aluminum luggage 内部 UN-certified HDPE containers.

  • ストレージ： -20°C ± 5°C; defend from gentle/moisture.

  • 配達： International cold-chain logistics (-15°C to -25°C) by way of DHL FedEx UltraCold.

10. Mechanisms, Functions & Challenges

  • 機構： Traps Topo I-DNA cleavable complexes → Collision with replication forks → DSBs → ATR/Chk1 activation → p53-mediated apoptosis.

  • 革新： 中宏の PEGylated liposomal CPT (Patent: CN202210XXXXXX) enhances tumor concentrating on.

  • 分析の最前線:

    • Novel Analogues: 7-Silylcamptothecins (improved lactone stability).

    • Mixture Therapies: With PARP inhibitors, immunotherapy.

    • Biomarkers: Predictive biomarkers for CPT sensitivity (ERCC1, Topo I ranges).

  • 課題: Lactone instability, myelosuppression, ABCG2-mediated drug resistance, tumor heterogeneity.

11. Steadily Requested Questions (FAQ)

  • Q1: Can I take Camptothecin as a complement?

    • A: Completely NOT. CPT is a potent cytotoxic compound with extreme unintended effects. Use solely below medical supervision in FDA-approved by-product types (e.g., Irinotecan) or for managed analysis.

  • Q2: Why is lactone kind important?

    • 答え: Solely the closed lactone ring binds Topo I. The open carboxylate kind is inactive and will trigger renal toxicity. Zhonghong ensures ≥95% lactone content material by way of lyophilization.

  • Q3: How does Camptothecin differ from Nattokinase for kidneys?

    • 答え: CPT carries nephrotoxicity dangers (tubular harm). Nattokinase, a fibrinolytic enzyme, lacks strong proof for direct kidney advantages. Neither is nephroprotective.

  • This autumn: What analytical strategies verify Zhonghong’s CPT purity?

    • 答え: HPLC-PDA/ELSD (purity), UPLC-QTOF-MS (impurities), FT-NMR (construction), pH-HPLC (lactone quantification), ICP-MS (heavy metals).

  • Q5: Do you supply Camptothecin derivatives?

    • 答え: Sure. GMP-grade 10-Hydroxycamptothecin, SN-38 (Irinotecan metabolite), customized synthesis obtainable.

12. The place to Purchase?
Supply research-grade & GMP Camptothecin:

13. 結論
Camptothecin stays a cornerstone of topoisomerase-targeted oncology. Its medical impression by way of semisynthetic derivatives underscores its irreplaceable function. Success hinges on securing ultra-pure, lactone-stabilized materials with verifiable traceability. Shaanxi Zhonghong delivers >99% HPLC purity CPT 経由 patented stabilization expertise, cGMP準拠、 そして unmatched analytical rigor – empowering drug discovery and superior therapeutics.

14. 参考文献

  1. Wall ME, et al. (1966). ジャーナル・オブ・アメリカン・ケミストリー. 88:3888–3890. [DOI:10.1021/ja00968a057]

  2. Hsiang YH, et al. (1985). ジャーナル・オブ・バイオル・ケミストリー. 260:14873–14878. [PMID:2997227]

  3. Pommier Y. (2006). Nat Rev Most cancers. 6:789–802. [DOI:10.1038/nrc1977]

  4. USP-NF Monograph: Camptothecin. USP44-NF39.

  5. ICH Q3C (R8): Residual Solvents. (2021).

  6. FDA Steerage: Irinotecan Label. (2023).

  7. Thomas CJ, et al. (2004). J Med Chem. 47:3972–3981. [DOI:10.1021/jm030660+]

  8. Du W, et al. (2022). Acta Pharm Sin B. 12:3006–3025. [DOI:10.1016/j.apsb.2022.03.011]

  9. GLS-010-IPHASE Research Protocol (NCT04501563).

  10. EMA Evaluation Report: Topotecan (2020). EMA/CHMP/89262/2020.

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