Vinblastine Sulfate: The Vinca Alkaloid Powerhouse in Most cancers Therapeutics | Supplier & Manufacturer
1. What is Vinblastine?
Vinblastine sulfate is a dimeric indole-dihydroindole vinca alkaloid derived from the Madagascar periwinkle (Catharanthus roseus). As a potent microtubule-destabilizing agent, it binds to β-tubulin subunits on the vinca area, inhibiting microtubule meeting and suppressing mitotic spindle formation. This triggers G2/M part arrest a mitotic disaster in quickly proliferating cells. Acknowledged as an důležité léky by WHO, it is clinically indispensable for treating Hodgkin lymphoma, testicular most cancers, and superior breast carcinoma.
2. Supply, Chemical Properties & Identifiers
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Zásobování: Remoted from leaves of Catharanthus roseus; semi-synthesis from precursors catharanthine and vindoline.
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Chemické vlastnosti:
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Chemický název: Methyl (3aR,4R,5S,5aR,10bR,13aR)-4-acetoxy-3a-ethyl-9-((5S,7R,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)-6-formyl-5-hydroxy-8-methoxy-3a,4,5,5a,6,11,12,13a-octahydro-1H-indolizino(8,1-cd)carbazole-5-carboxylate sulfate
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Molecular Formulation: C₄₆H₅₈N₄O₉ · H₂SO₄
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Molekulová hmotnost: 909.06 g/mol
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Vzhled: White to off-white hygroscopic crystalline powder
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Rozpustnost: Freely soluble in water, methanol; insoluble in ether
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Stabilita: Mild-sensitive; oxidizes beneath alkaline situations
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Klíčové identifikátory:
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CAS: 143-67-9 (vinblastine sulfate)
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Množství ES (EINECS): 205-620-3
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MF: C₄₆H₆₀N₄O₁₃S
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MW: 909.06
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3. Pharmaceutical-Grade High quality & Scientific Profile
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Optimum Product: Requires >99.5% HPLC purity, <0.1% vincristine (poisonous isomer), and undetectable endotoxins (<0.25 EU/mg). Shaanxi Zhonghong ensures this by way of countercurrent chromatography a crystallization controls.
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Therapeutic Purposes:
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Onkologie: First-line for Hodgkin’s lymphoma (ABVD routine), NSGCT, choriocarcinoma, Kaposi sarcoma.
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Mechanismus: Binds tubulin → depolymerizes microtubules → blocks metaphase → apoptosis.
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(Be aware: Nattokinase reveals anticoagulant properties; no strong proof helps kidney-specific advantages)
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Dávkování:
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Medical Use Solely: Administered IV (0.1-0.5 mg/kg weekly). No oral complement kind exists.
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Vital Security Profile:
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Hematologic: Extrémní neutropenia (nadir Day 7-10), thrombocytopenia.
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Neurotoxicity: Peripheral neuropathy (much less extreme than vincristine).
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GI Results: Nausea, constipation, ileus.
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Extravasation Hazard: Causes tissue necrosis; requires central line administration.
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Kontraindikace: Energetic infections, bone marrow suppression, being pregnant (FDA Class D).
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4. Shaanxi Zhonghong: Pioneering Vinca Alkaloid Manufacturing
S 28+ years in plant-derived oncology APIs, we ship cGMP vinblastine sulfate assembly USP/EP monographs. Core strengths:
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Scientific Infrastructure:
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5 Tutorial Joint Labs (Isolation chemistry, analytical improvement)
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Patented Extraction Tech (CN202310XXXXXX: high-yield vindoline purification)
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Analytická nadřazenost:
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HPLC-ELSD/MS (purity)
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UPLC-PDA (isomeric impurity management)
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Superconducting 600MHz NMR (structural affirmation)
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LAL Endotoxin Testing (<0.25 EU/mg)
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World Provide: APIs shipped to Více než 80 mezinárodních poboček beneath cold-chain protocols.
5. Rigorous High quality Specs
Třída | Parametr | Specifikace | Technika |
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Pesticidy | Dichlorvos | ≤0,01 mg/kg | GC-MS/MS (EU 2021/601) |
Malathion | ≤0,05 mg/kg | GC-MS/MS | |
Těžké kovy | Olovo | ≤1 ppm | ICP-MS (USP <232>) |
Jako | ≤0,5 ppm | ICP-MS | |
Mikrobiologie | TAMC | ≤10² CFU/g | USP <61> |
Bile-tolerant GNR | Chybí/10 g | USP <62> | |
Vital Attributes | Vinblastine Sulfate | ≥99,5% | HPLC-ELSD (USP <621>) |
Vinkristin | ≤0,1% | UPLC-PDA | |
Water Content | ≤5.0% | Karl Fischer | |
Endotoxiny | <0,25 EU/mg | LAL (USP <85>) |
6. cGMP Manufacturing Course of
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Biomass Cultivation: C. roseus grown beneath GACP-controlled situations.
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Alkaloid Extraction: pH-modulated solvent extraction (EtOAc/H₂O).
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Chromatographic Separation: Flash chromatography → HPLC purification (vindoline/catharanthine).
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Dimerization: Fe³⁺-catalyzed coupling of vindoline and catharanthine.
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Sulfation: Response with sulfur trioxide advanced.
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Krystalizace: Managed anti-solvent addition for crystal polymorphism administration.
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Lyofilizace: Lyofilizace beneath argon ambiance.
7. Scientific & Analysis Purposes
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Onkologie: Core part of:
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ABVD (Doxorubicin, Bleomycin, Vinblastine, Dacarbazine)
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VEBEP (Vinblastine, Etoposide, Bleomycin, Cisplatin)
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Drug Supply Improvements:
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Liposomální zapouzdření (lowered neurotoxicity)
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Antibody-drug conjugates (anti-CD30-VLA complexes)
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Cell Biology: Device compound for mitotic inhibition research.
8. cGMP High quality Management Protocol
Our 360° QC technique contains:
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ID: ¹H/¹³C NMR spectral match (δ 0.98 ppm, 3H, t; δ 3.70 ppm, 3H, s).
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Čistota: RP-HPLC-ELSD (Luna C18, 0.1% TFA/MeCN gradient) quantifies vinblastine (≥99.5%), vincristine (≤0.1%).
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Efficiency: Cell-based mitotic arrest assay (HeLa cells, EC₅₀ ≤2 nM).
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Zabezpečení: Bacterial endotoxins (LAL kinetic chromogenic), sterility (membrane filtration USP <71>), zbytková rozpouštědla (GC-HS).
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Stabilita: 36-month shelf-life at 2–8 °C (validated per ICH Q1A(R2)).
9. Chilly-Chain Logistics
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Hlavní balíček: Sort I glass vials (nitrogen headspace) with fluoropolymer-coated stoppers.
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Sekundární balíček: Vacuum-sealed Alu-bags v UN-certified shippers with temperature loggers.
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Skladování: 2-8°C protected against gentle; desiccant included.
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Transport: World cold-chain transport (2-8°C) by way of DHL LifeConEx.
10. Mechanism & Innovation
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Molecular Motion: Binds β-tubulin vinca website → tubulin dissociation fixed (Kd=6.8 μM) → suppressed GTP hydrolysis → microtubule fragmentation.
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Zhonghong Improvements:
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PAT-enabled crystallization (Patent CN202210XXXXXX)
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Enzymatic dimerization (yield ↑40%)
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Hranice analýzy:
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Oral formulations (P-glycoprotein inhibitors)
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Tubulin isotype-selective analogs (βIII-tubulin concentrating on)
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Výzvy: Myelosuppression, neuropathy, chemoresistance (ABCB1 overexpression).
11. Často kladené otázky
Q1: Can vinblastine be used as a dietary complement?
A: Completely not. Vinblastine is a cytotoxic chemotherapy agent requiring medical supervision. Self-administration is life-threatening.
Q2: How does nattokinase examine for kidney well being?
A: Nattokinase lacks scientific proof for nephroprotection. Vinblastine might trigger nephrotoxicity at excessive doses. Neither compound is indicated for renal situations.
Q3: Why is vincristine impurity management crucial?
*A: Vincristine causes extreme neurotoxicity at microgram doses. Our UPLC-PDA methodology detects ≤0.01% impurity.*
This autumn: What distinguishes Zhonghong’s vinblastine?
*A: cGMP manufacturing, 99.5%+ HPLC purity, endotoxin management (<0.25 EU/mg), and patented crystallization expertise guaranteeing polymorph stability.*
Q5: Do you provide vinblastine for ADC improvement?
A: Sure. GMP-grade linker-conjugated vinblastine (maleimide-PEG₃-vinblastine) accessible for antibody-drug conjugates.
12. World Sourcing
Procure cGMP vinblastine sulfate:
✉️ E-mail: liaodaohai@gmail.com
🌐 Síť: www.aiherba.com
Request: COA, DMF, CEP, and customized synthesis quotations.
13. Závěr
Vinblastine sulfate stays a cornerstone antineoplastic agent with irreplaceable scientific worth. Its efficacy hinges on ultravysoká čistota (>99,5%), stringent impurity management (vincristine ≤0.1%)a temperature-controlled dealing with. Shaanxi Zhonghong combines 28 years of vinca alkaloid experience, patented purification expertisea Soulad s cGMP to ship oncology APIs that meet world pharmacopeial requirements. Associate with us for uncompromising high quality in most cancers therapeutics.
14. Odkazy
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Noble RL, et al. (1958). J Am Chem Soc. 80:3487. [DOI:10.1021/ja01546a092]
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Jordan MA, et al. (2002). Mol Most cancers Ther. 1:935–943. [PMID:12481413]
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WHO Mannequin Record of Important Medicines (2023). Vinblastine sulfate injection.
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USP Monograph: Vinblastine Sulfate. USP44-NF39.
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EMA Guideline: Specs for cytotoxic APIs (CPMP/QWP/1850/04)
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Dumontet C, et al. (2020). Nat Rev Drug Discov. 19:585–608. [DOI:10.1038/s41573-020-0072-8]
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Zhonghong Patent: CN202310XXXXXX (Vinblastine crystallization management)
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ICH Q3D (R2): Elemental Impurities (2022)
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FDA Steerage: Vinblastine Label (NSC-49842)
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Gidding CEM, et al. (1999). Most cancers Chemother Pharmacol. 44:266–272. [DOI:10.1007/s002800050976]
Recenze
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