5-Azacytidine | CAS 320-67-2 | 98% Purity (HPLC) | White to Almost White Crystalline Powder | Antitumor Epigenetic Agent & DNA Methyltransferase Inhi

1. Product Overview

5-Azacytidine, CAS 320-67-2, also known as Azacitidine, Ladakamycin, or Mylosar, is a pyrimidine nucleoside analog of cytidine with molecular formula C₈H₁₂N₄O₅ and MW 244.20 g/mol. It appears as a white to almost white crystalline powder at room temperature, freely soluble in water (~187 mg/mL at 25°C), slightly soluble in methanol, and practically insoluble in non-polar solvents. This compound is a potent DNA methyltransferase inhibitor that incorporates into RNA and DNA, leading to covalent trapping of DNMTs and global DNA demethylation. It is light-sensitive, hygroscopic, and thermally labile (decomposes around 228–230°C). Widely used in epigenetics research, oncology drug development, and as a pharmaceutical intermediate (API for myelodysplastic syndromes/AML).

2. Key Features and Advantages

• Epigenetic Modulator — First-in-class DNMT inhibitor; induces DNA hypomethylation and reactivates silenced tumor-suppressor genes.

• High Purity Grades — Available as ≥98% HPLC for research, USP/EP-compliant API grade for clinical use, and isotopically labeled variants (e.g., ¹⁵N₄).

• Dual Incorporation — Incorporates into both RNA (primarily) and DNA, enabling broad epigenetic and transcriptional studies.

• Well-Characterized Pharmacolog — Established PK/PD profile; standard reference in epigenetic screening and MDS/AML therapy.

• Stability-Optimized Packaging — Supplied in amber vials under inert atmosphere, lyophilized or desiccated for extended shelf life.

3. Main Applications

5-Azacytidine is deployed across epigenetics and pharma sectors: Epigenetics Research (DNA methylation/demethylation studies, chromatin remodeling assays, cell line reprogramming/iPSC generation); Oncology / Hematology (API for myelodysplastic syndromes (MDS), acute myeloid leukemia (AML), chronic myelomonocytic leukemia; preclinical antitumor screening); Pharmaceutical Intermediate (synthesis of modified nucleosides, labeled tracers, and next-gen epigenetic drug candidates); Cell Biology (low-dose treatment to induce pluripotency in somatic cells; global hypomethylation protocols); Analytical Reference (USP/EP pharmacopeial standard for assay validation, QC testing of azacitidine drug products).

4. Technical Specifications

5. Storage and Handling

• Storage Conditions: Store in a cool, dark, dry place under inert atmosphere (N₂ or Ar). Recommended: −20°C in amber vials, desiccated, protected from light. For long-term: lyophilized powder at −20°C to −80°C; avoid repeated freeze-thaw cycles.

• Packaging Options: Research: 20 mg / 100 mg / 250 mg / 1 g / 5 g amber glass vials with septa; API: 100 mg USP vial, 1 g / 5 g / 25 g / 100 g / 500 g / 1 kg foil-pouched under argon; bulk API: 1 kg / 5 kg / 25 kg drums (custom synthesis).

• Shelf Life: ≥24 months when stored unopened at −20°C, desiccated and protected from light; reconstituted solutions stable ≤24 h at 2–8°C.

• Handling Precautions: Use in fume hood with low-light conditions (amber lighting or dimmed). Wear nitrile gloves, safety goggles, lab coat. Avoid inhalation of powder; handle as cytotoxic/teratogenic agent. Use desiccator and weigh quickly to limit moisture uptake.

• Incompatible Materials: Strong oxidizers, acids/bases causing hydrolysis, prolonged UV/visible light exposure.

6. Safety Overview

GHS pictograms: GHS06 (Skull & Crossbones), GHS07 (Exclamation), GHS08 (Health Hazard). Signal word: Warning / Danger (API-grade). Hazard statements: H300+H310+H330 (fatal if swallowed/in contact with skin/if inhaled — cytotoxic/nucleoside analog); H315 (skin irritant); H319 (eye irritant); H341 (suspected of causing genetic defects); H360 (may damage fertility or unborn child). Precautionary: P201/P261/P264/P270/P271/P280/P284/P301+P310/P305+P351+P338/P308+P313. Acute toxicity: cytotoxic in vitro at nM–μM range; animal LD₅₀ oral ~200–400 mg/kg (rat). Transport: Non-hazardous for small research packs; API bulk may be UN2811 (Toxic Solid, Organic, n.o.s.), PG III. Regulatory: USP Reference Standard available; controlled for clinical/API use; for research only unless GMP-certified. Dispose as cytotoxic/hazardous chemical waste per local regs. In case of contact: skin—wash thoroughly; eyes—rinse 15 min + medical aid; ingestion—do NOT induce vomiting, seek immediate medical attention.