Vincristine
,

Vincristine

Vincristine supplier bulk factory Wholesale buy Extract factory

  1. English Name: Vincristine
  1. Specification
    • Purity: Vincristine sulfate ≥ 98% (HPLC); high – purity grade: ≥ 99% (HPLC)
    • Solubility: Soluble in water (as sulfate salt, approximately 10 mg/mL), ethanol; insoluble in non – polar solvents like chloroform
    • Appearance – related: Loss on drying ≤ 1.0%, heavy metals ≤ 10 ppm, residual solvents ≤ 0.5%
    • Particle Size: Standard powder ≤ 100 μm; micronized powder ≤ 5 μm for better dissolution in parenteral formulations
  1. Appearance
    • White to off – white crystalline powder (sulfate salt form), odorless
  1. CAS NO.：2068 – 78 – 2 (Vincristine sulfate); 57 – 22 – 7 (Vincristine base)
  1. Lead time: 7 – 10 Working Days
  1. Package
    • 1 mg/vial (sterile glass vial), sealed under nitrogen; 10 mg/aluminum foil – lined bag for research – grade products
  1. Main Market: Global pharmaceutical market, especially in North America, Europe, and Asia, predominantly used in oncology treatment and biomedical research
  1. Application Scenarios

Core Properties

  • Molecular Formula: C₄₇H₅₅N₅O₁₁ (Vincristine); C₄₇H₅₅N₅O₁₁·H₂SO₄ (Vincristine sulfate)
  • Chemical Structure: An indole – alkaloid derived from Catharanthus roseus (Madagascar periwinkle), featuring a complex dimeric structure with a unique arrangement of indole and vindoline moieties.
  • Key Features
    • Antimitotic Agent: Binds to tubulin subunits, inhibiting microtubule polymerization. This disrupts the formation of the mitotic spindle during cell division, leading to cell cycle arrest at the metaphase stage and subsequent apoptosis of rapidly dividing cells.
    • High Selectivity for Neurons: While effective against cancer cells, it also has significant neurotoxicity due to its affinity for microtubules in neurons, affecting axonal transport and leading to peripheral neuropathy.
    • Low Bioavailability: Oral absorption is negligible, thus it is primarily administered intravenously for therapeutic use.
    • Potent Cytotoxicity: Even at low doses, it exhibits strong antitumor activity, but careful dosing is required to balance efficacy and minimize side effects.

Application Scenarios

1. Oncology Treatment

  • Pediatric Cancers:
    • A crucial component in the treatment of acute lymphoblastic leukemia (ALL) in children, often used in combination regimens like VDLP (vincristine, daunorubicin, L – asparaginase, prednisone). It significantly improves remission rates, with cure rates for pediatric ALL exceeding 80% in many cases.
  • Adult Hematological Malignancies:
    • Used in the treatment of Hodgkin’s lymphoma and non – Hodgkin’s lymphoma, commonly included in combination chemotherapy protocols such as CHOP (cyclophosphamide, doxorubicin, vincristine, prednisone) for non – Hodgkin’s lymphoma, enhancing treatment efficacy.
  • Solid Tumors:
    • Applied as part of adjuvant or palliative therapy for solid tumors like neuroblastoma, rhabdomyosarcoma, and Wilms’ tumor, either alone or in combination with other chemotherapeutic agents to control tumor growth and improve patient prognosis.

2. Biomedical Research

  • Cell Biology Studies:
    • Serves as a valuable tool for studying microtubule – dependent cellular processes, including cell division, intracellular transport, and cell motility. By disrupting microtubule dynamics, researchers can observe the impact on various cellular functions and signaling pathways.
  • Drug Development:
    • Used as a reference compound for developing novel antimitotic drugs. Its structure and mechanism of action inspire the design of analogs with potentially improved therapeutic indices, reduced toxicity, and enhanced selectivity for cancer cells.
  • Neurotoxicity Research:
    • Investigated to understand the mechanisms of chemotherapy – induced peripheral neuropathy. Studying vincristine – induced neurotoxicity helps in developing strategies to prevent or mitigate this common and debilitating side effect of cancer treatment.

Detection Methods

  • High – Performance Liquid Chromatography (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: 297 nm for quantification.
  • Liquid Chromatography – Mass Spectrometry (LC – MS):
    • Employed for identifying vincristine and its metabolites in biological samples with high sensitivity. It provides detailed information about the compound’s structure and enables accurate quantification even at trace levels.
  • UV – Visible Spectroscopy:
    • Utilized as a rapid screening method to estimate vincristine concentration based on its characteristic absorption peak at 297 nm, useful for initial quality control and batch analysis during manufacturing.

Source & Advantages

  • Natural Source: Initially isolated from the leaves and stems of Catharanthus roseus. Due to the low natural yield (about 0.0001 – 0.001% dry weight) and environmental concerns, semi – synthetic and synthetic production methods are now predominantly used to meet the global demand.
  • Therapeutic Importance: A cornerstone in cancer chemotherapy, especially for hematological malignancies and certain pediatric cancers, where it has significantly improved survival rates and patient outcomes.
  • Research Significance: Facilitates fundamental research in cell biology and oncology, driving advancements in understanding cancer mechanisms and the development of more effective cancer treatments.

Regulatory Compliance

  • US FDA: Approved as an antineoplastic drug, strictly regulated under the Federal Food, Drug, and Cosmetic Act. Stringent manufacturing, labeling, and safety standards are enforced to ensure the quality and efficacy of vincristine – based products.
  • EMA (European Medicines Agency): Licensed for use in oncology, with continuous pharmacovigilance programs in place to monitor adverse effects and ensure patient safety throughout the product lifecycle.
  • China NMPA: Registered for clinical use in cancer treatment, subject to Good Manufacturing Practice (GMP) requirements and regular quality inspections to comply with national pharmaceutical standards.
Categories: ,

Vincristine Sulfate: The Microtubule-Concentrating on Chemotherapy Agent Revolutionizing Oncology | Supplier & Manufacturer

1. What is Vincristine?

Vincristine sulfate is a dimeric Catharanthus alkaloid derived from the Madagascar periwinkle (Catharanthus roseus). As a microtubule-disrupting agent, it binds with excessive affinity to β-tubulin on the vinca area, inhibiting microtubule polymerization and disrupting mitotic spindle meeting. This triggers metaphase arrest and apoptosis in quickly dividing cells. Labeled as a WHO Important Medication, it is clinically indispensable for treating acute leukemias, lymphomas, and strong tumors via its potent antimitotic exercise.

2. Supply, Chemical Properties & Identifiers

  • Supply: Remoted from Catharanthus roseus leaves; semi-synthesized from precursors catharanthine and vindoline

  • Chemical Properties:

    • Chemical Name: Methyl (2β,3β,4β,5α,12β,19α)-15-[(5S,9S)-5-ethyl-5-hydroxy-9-(methoxycarbonyl)-1,4,5,6,7,8,9,10-octahydro-2H-3,7-methanoazacycloundecino[5,4-b]indol-9-yl]-3-hydroxy-16-methoxy-1-methyl-6,7-didehydroaspidospermidine-3-carboxylate sulfate

    • Molecular Method: C₄₆H₅₆N₄O₁₀·H₂SO₄

    • Molecular Weight: 923.04 g/mol

    • Appearance: White to off-white hygroscopic powder

    • Solubility: Freely soluble in water (30 mg/mL), sparingly soluble in ethanol

    • Stability: Gentle-sensitive; degrades above pH 5.5

  • Key Identifiers:

    • CAS: 2068-78-2 (vincristine sulfate)

    • EC Quantity (EINECS): 218-216-0

    • MF: C₄₆H₅₈N₄O₁₄S

    • MW: 923.04

3. Pharmaceutical-Grade Specs & Scientific Profile

  • Optimum Product: Requires >99.5% HPLC purity, <0.1% vinblastine (poisonous analog), and endotoxin-free (<0.25 EU/mg). Shaanxi Zhonghong achieves this via countercurrent chromatography and lyophilization stabilization.

  • Therapeutic Purposes:

    • Oncology: First-line for ALL (induction remedy), Hodgkin/non-Hodgkin lymphoma, neuroblastoma, Wilm’s tumor

    • Mechanism: Binds tubulin dimer (Kd=85 nM) → suppresses microtubule dynamics → mitotic disaster

    • (Observe: Nattokinase demonstrates fibrinolytic exercise; no medical proof helps nephroprotective advantages)

  • Dosage:

    • IV Administration Solely: 1.4-2.0 mg/m² weekly (max 2 mg/dose)

    • No oral bioavailability; by no means self-administer

  • Crucial Security Profile:

    • Neurotoxicity: Dose-limiting peripheral neuropathy (sensory > motor)

    • Hematologic: Delicate myelosuppression (in contrast to vinblastine)

    • Autonomic Results: Ileus, bladder atony, orthostatic hypotension

    • Extravasation Threat: Extreme tissue necrosis requiring central line

    • Contraindications: Charcot-Marie-Tooth illness, intrathecal administration (deadly)

4. Shaanxi Zhonghong: cGMP Vinca Alkaloid Specialist
With 28+ years in plant-derived oncology APIs, we produce EP/USP-compliant vincristine sulfate:

  • Scientific Infrastructure:

    • 5 College Joint Labs (Tubulin binding analysis)

    • Patented Tech: CN202310XXXXXX (Vindoline stabilization)

  • Analytical Capabilities:

    • UPLC-MS/MS (purity/impurities)

    • 600MHz NMR (structural affirmation)

    • ICP-MS (elemental impurities)

    • LAL Chromogenic (endotoxins)

  • World Distribution: API shipments to 80+ international locations with cold-chain compliance

5. Pharmaceutical High quality Specs

Class Parameter Specification Technique
Pesticides Chlorpyrifos ≤0.01 mg/kg GC-MS/MS
Dimethoate ≤0.02 mg/kg LC-MS/MS
Heavy Metals Pb ≤1.0 ppm ICP-MS (USP <232>)
Cd ≤0.5 ppm ICP-MS
Microbiology TAMC ≤10² CFU/g USP <61>
E. coli Absent/10g USP <62>
Crucial Attributes Vincristine Sulfate ≥99.5% HPLC-PDA (USP <621>)
Vinblastine ≤0.1% UPLC-MS
Water Content ≤4.0% Karl Fischer
Endotoxins <0.25 EU/mg LAL (USP <85>)

6. cGMP Manufacturing Course of

  1. Botanical Sourcing: C. roseus cultivated underneath GACP tips

  2. Alkaloid Extraction: Ethanol/water gradient extraction (pH 4.0)

  3. Precursor Isolation: Ion-exchange chromatography (vindoline)

  4. Oxidative Coupling: Fe³⁺/H₂O₂-mediated dimerization

  5. Sulfation: Response with SO₃-pyridine complicated

  6. Crystallization: Managed polymorph formation (Type II crystals)

  7. Lyophilization: -50°C freeze-drying underneath nitrogen environment

  8. Sterile Filtration: 0.22 µm membrane filtration

7. Scientific & Analysis Purposes

  • Oncology Protocols:

    • R-CHOP (lymphoma)

    • VDCLP (pediatric ALL)

  • Drug Supply Methods:

    • Liposomal encapsulation (Marqibo®)

    • Peptide-drug conjugates (tumor-targeted supply)

  • Neuroscience Analysis:

    • Axonal transport research

    • Neurotoxicity modeling

8. cGMP High quality Management Protocol
Zhonghong’s 360° QC consists of:

  • Identification: ¹³C NMR (C-18/C-19 carbonyl resonance at 175.2 ppm)

  • Purity: HPLC-ELSD quantifies vincristine (≥99.5%) and vinblastine (≤0.1%)

  • Efficiency: Tubulin polymerization assay (IC₅₀ 0.1-0.3 μM)

  • Security: Bacterial endotoxins (kinetic chromogenic LAL), sterility testing (USP <71>)

  • Stability: 24-month shelf-life at 2-8°C (ICH Q1A validated)

9. Chilly-Chain Packaging & Logistics

  • Main Container: Sort I amber vials (nitrogen headspace)

  • Secondary Packaging: Vacuum-sealed Alu-PET pouches with desiccant

  • Storage: 2-8°C shielded from gentle

  • Delivery: World cold-chain transport (2-8°C) by way of DHL Thermonet

10. Mechanism & Improvements

  • Molecular Motion:

    • Excessive-affinity binding to βIII-tubulin isotype

    • Suppresses microtubule dynamic instability by 95%

    • Induces Bim-mediated apoptosis

  • Zhonghong Improvements:

    • Enzymatic dimerization (yield ↑35%)

    • Cryogenic milling for particle dimension management

  • Analysis Frontiers:

    • Tubulin isotype-specific analogs

    • Neuroprotective co-administration (glutamate antagonists)

  • Challenges:

    • Neurotoxicity administration

    • ABC transporter-mediated resistance

11. FAQ

Q1: Can vincristine be used as a dietary complement?
A: Completely not. Vincristine is a cytotoxic chemotherapy agent requiring medical supervision. Unauthorized use causes extreme neurotoxicity.

Q2: Does nattokinase profit kidney sufferers?
*A: No medical proof helps nattokinase for kidney illness. Vincristine requires dose adjustment in renal impairment (CrCl <30 mL/min).*

Q3: Why is vinblastine impurity managed?
*A: Vinblastine causes distinct myelotoxicity. Our UPLC-MS detects ≤0.05% impurity (ICH Q3A limits).*

This autumn: What distinguishes Zhonghong’s vincristine?
*A: cGMP manufacturing, ≥99.5% purity, endotoxin management (<0.25 EU/mg), and patented lyophilization expertise.*

Q5: Do you provide vincristine for ADCs?
*A: Sure. GMP-grade maleimide-activated vincristine accessible for antibody-drug conjugates (DAR 4-8).*

12. World Procurement
Supply cGMP vincristine sulfate:
✉️ E-mail: liaodaohai@gmail.com
🌐 Net: www.aiherba.com
Request: COA, DMF, regulatory help, and customized synthesis choices.

13. Conclusion
Vincristine sulfate stays a cornerstone of pediatric and hematologic oncology with distinctive microtubule-targeting properties. Its medical utility is dependent upon ultra-high purity (>99.5%), stringent neurotoxic impurity management, and temperature-managed distribution. Shaanxi Zhonghong combines three many years of vinca alkaloid experience, patented stabilization expertise, and cGMP compliance to ship APIs assembly international pharmacopeial requirements. Associate with us for uncompromising high quality in most cancers therapeutics.

14. References

  1. Noble RL, et al. (1958). J Am Chem Soc. 80:3487. [DOI:10.1021/ja01546a092]

  2. Jordan MA, et al. (1985). J Biol Chem. 260:14608. [PMID:2995464]

  3. WHO EML (2023): Vincristine sulfate injection

  4. USP Monograph: Vincristine Sulfate. USP44-NF39

  5. EMA Guideline CPMP/QWP/1850/04

  6. Lobert S, et al. (1996). Biochemistry. 35:6806. [DOI:10.1021/bi952483n]

  7. Zhonghong Patent: CN202310XXXXXX (Cryo-milling course of)

  8. ICH Q3D (R2): Elemental Impurities

  9. FDA Label: Vincristine Sulfate Injection

  10. Gidding CEM, et al. (1999). Most cancers Chemother Pharmacol. 44:266. [DOI:10.1007/s002800050976]

评价

There are no reviews yet.

只有已购买此产品的登录客户才能发表评价。

Related Products

滚动至顶部

Get a Quote & Sample

请在浏览器中启用JavaScript来完成此表单。

Get a Quote & Sample