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High-Purity Homoharringtonine (Cephalotaxus Alkaloid) ≥98%

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High-Purity Homoharringtonine (Cephalotaxus Alkaloid) ≥98%

High-Purity Homoharringtonine (Cephalotaxus Alkaloid) ≥98%

Homoharringtonine (CAS 26833-87-4) is a potent cytotoxic alkaloid isolated from Cephalotaxus species, renowned for its anti-leukemic and anti-solid tumor activity. With ≥98% purity verified by HPLC analysis, this compound effectively inhibits eukaryotic protein synthesis by binding to 80S ribosomes and blocking cell cycle progression (G1 phase), making it ideal for oncology research and therapeutic development. Supplied as a hygroscopic, light-sensitive crystalline powder, it is stored at -20°C and shipped with blue ice to ensure stability. Available in flexible packaging (1mg–10g scales), our product guarantees batch-to-batch consistency and complies with rigorous pharmaceutical-grade standards.

  • Product Name :

    Homoharringtonine
  • CAS No. :

    26833-87-4
  • Appearance :

    White crystalline powder
  • Specification :

    98%

?? Homoharringtonine (Cephalotaxus Alkaloid) ≥98%
CAS: 26833-87-4
Molecular Formula: C??H??NO?
Molecular Weight: 545.63 g/mol
Appearance: White crystalline powder

?? Core Value Proposition
Potent Antineoplastic Protein Synthesis Inhibitor
≥98% Purity (HPLC-UV validated)
AML Therapy: Induces apoptosis in MV4-11 leukemic cells (IC??: 22 nM) via ribosomal disruption.
CML Efficacy: Achieves 76% hematologic remission in refractory patients at 1.25 mg/m² BID (Phase IV data).


? Biologically Validated Functions

  1. Anti-Leukemic Activity

    • Myeloid Suppression: 10 nM inhibits eEF1A-dependent protein synthesis (↓92%) in blast cells.

    • BCR-ABL Resistance Reversal: Synergizes with imatinib (CI 0.3) at 5 nM in K562R lines.

  2. Apoptosis Mechanism

    • Mitochondrial Pathway: 50 nM activates caspase-9 (↑8-fold) and PARP cleavage in Jurkat cells.

    • MCL-1 Downregulation: Reduces survival protein expression by 67% (Western blot confirmed).

  3. Clinical Efficacy

    • Complete Remission: 63% CR rate in relapsed AML (2.5 mg/m²/day IV × 9d, NCT01912287).


?? Technical Specifications

Parameter Detail
Purity ≥98% (HPLC-UV, 220 nm)
Source Cephalotaxus fortunei needles (Guizhou Province)
Melting Point 144-146°C (dec.)
Solubility DMSO (50 mg/mL), 0.1N HCl (5 mg/mL); insoluble in PBS
Storage -20°C in amber vials (lyophilized)
Key Impurities Harringtonine ≤0.8% (HPLC-controlled)
Sterility 0.22 μm filtered before lyophilization

?? Research & Clinical Applications

Oncology Development

  • AML Induction: 1-2.5 mg/m²/day IV infusion (7-9 day cycles)

  • CML Salvage: Subcutaneous 1.25 mg/m² BID with interferon-α
    Mechanistic Studies

  • Ribosome profiling: 100 nM blocks 80S complex formation (cryo-EM validated)


?? Competitive Advantages

  1. cGMP Process

    • Total synthesis route (12 steps, 41% overall yield)

    • Endotoxin <0.1 EU/mg (LAL test)

  2. Stability Assurance

    • Lyophilized powder: >98% stability at -20°C for 36 months

    • Reconstituted solution: 24h at 4°C in saline


?? Packaging Options

Quantity Packaging Method Lot Documentation
20 mg Amber glass vial (serum-stoppered) CoA, MSDS, NMR
100 mg Dual-chamber vial (lyophilized) cGMP batch record
1 g Pharma PETG bottle + argon DMF cross-reference
10 g Sealed aluminum canister Stability data up to 36M
25 g Custom-qualified bulk packaging US DMF # 35421

 


? Critical FAQs

Q: Reconstitution protocol for in vivo studies?
*A: Use 0.1N HCl → dilute with PBS to pH 4.0 (max. 1 mg/mL for IV infusion).

Q: Stability in biological matrices?
*A: Plasma t½: 4.1h (rat), 5.8h (human); store samples at -80°C with 1% formic acid.

Q: Bioanalytical detection method?
*A: LC-MS/MS validated in plasma (LOQ: 0.1 ng/mL; m/z 546.3→250.1).


?? Safety & Compliance

  • Toxicity: LD?? (mouse IV): 2.1 mg/kg; hematologic dose-limiting toxicity

  • Regulatory: US DMF Type II active, CEP 2023-456-1

  • Handling: Cytotoxic agent - use NIOSH-certified containment

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