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MilliporeSigma

SML4376

MFS03

≥98% (HPLC)

Synonym(s):

4-(2-(3-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)propanamido)ethyl)phenyl sulfurofluoridate

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About This Item

Empirical Formula (Hill Notation):
C15H15FN2O6S
CAS Number:
Molecular Weight:
370.35
UNSPSC Code:
12352200
Assay:
≥98% (HPLC)
Form:
powder
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Quality Segment

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

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.


Storage Class

11 - Combustible Solids

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable



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