SML4376

MFS03

≥98% (HPLC)

• Synonym(e): 4-(2-(3-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)propanamido)ethyl)phenyl sulfurofluoridate
• Empirische Formel (Hill-System): C₁₅H₁₅FN₂O₆S
• CAS-Nummer: 3089116-28-6
• Molekulargewicht: 370.35
• UNSPSC Code: 12352200
• Assay: ≥98% (HPLC)
• Form: powder

Eigenschaften

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: -10 to -25°C

Beschreibung

Biochem/physiol Actions

The MFS03 (maleimido fluorosulfonyl) linker is a heterobifunctional covalent tether that converts affinity proteins (affibody and monobody) into irreversible therapeutics. MFS03 features a maleimide for cysteine conjugation and a bio-orthogonal aryl fluorosulfate warhead on a flexible spacer (2.92–17.7 Å), which initiates a proximity-enabled Sulfur(VI) Fluoride Exchange (SuFEx) reaction with target nucleophiles like histidine or lysine. On HER2/EGFR scaffolds, this covalent anchoring enhances therapeutic performance, yielding >2-fold tumor retention, 185% higher cellular uptake, and near-complete tumor inhibition. This permanent binding decouples pharmacodynamics from pharmacokinetics, boosting cytotoxicity 2.5- to 4.9-fold (to 0.31 nM) while maintaining a favorable biosafety profile.

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable