1059477-92-7

Upstream product

• 125797-57-1 N¹⁰-TFA-pteroic acid 
• 1227510-37-3 3,4;5,6-di-O-isopropylidene-1-amino-1-deoxy-(Fmoc-Glu-OH)-D-glucitol 
• 84793-07-7 Fmoc-Glu-OtBu 
• 71989-18-9 Fmoc-Glu(OtBu)-OH 
• 37793-53-6 N¹⁰-(trifluoroacetyl)pteroic acid 
• 71989-14-5 Fmoc-(tBu)Asp-OH 
• 104091-08-9 Fmoc-Glu(OtBu)-OH 

Relevant academic research and scientific papers

Conjugates containing hydrophilic spacer linkers

Described herein are compositions and methods for use in targeted drug delivery using cell receptor binding drug delivery conjugates containing hydrophilic spacer linkers for use in imaging, diagnosing, and/or treating diseases and disease states caused by pathogenic cell populations.

Binding ligand linked drug delivery conjugates of tubulysins

Described herein are compounds, pharmaceutical compositions, and methods for treating pathogenic cell populations. Kits including the compounds or pharmaceutical compositions are described. The compounds described herein include conjugates of tubulysins a

VITAMIN RECEPTOR DRUG DELIVERY CONJUGATES FOR TREATING INFLAMMATION

Described herein are compositions, methods, compounds, conjugates, and kits for use in targeted drug delivery using drug delivery conjugates containing hydrophilic spacer linkers for use in treating disease states caused by pathogenic cell populations, such as inflammatory cells.

Carbohydrate-based synthetic approach to control toxicity profiles of folate-drug conjugates

Figure presented To better regulate the biodistribution of the vinblastine-folate conjugate, EC145, a new folate-spacer that incorporates 1-amino-1-deoxy-d-glucitol-γ-glutamate subunits into a peptidic backbone, was synthesized. Synthesis of Fmoc-3,4;5,6-di-O-isopropylidene-1-amino-1-deoxy- d-glucitol-γ-glutamate 20, suitable for Fmoc-strategy solid-phase peptide synthesis (SPPS), was achieved in four steps from δ-gluconolactone. Addition of alternating glutamic acid and 20 moieties onto a cysteine-loaded resin, followed by the addition of folate, deprotection, and cleavage, resulted in the isolation of the new folate-spacer: Pte-γGlu-(Glu(1-amino-1-deoxy- d-glucitol)-Glu)2-Glu(1-amino-1-deoxy-d-glucitol)-Cys-OH (21). The addition of 21 to an appropriately modified desacetylvinblastine hydrazide (DAVLBH) resulted in a conjugate (25) with an improved therapeutic index. Treatment of 25 with DTT in neutral buffer at room temperature demonstrated that free DAVLBH would be released under the reductive environment of the internalized endosome.

BINDING LIGAND LINKED DRUG DELIVERY CONJUGATES OF TUBULYSINS

Described herein are compounds, pharmaceutical compositions and methods for treating pathogenic cell populations. The compounds described herein include conjugates of tubulysins and vitamin receptor binding ligands. The conjugates also include a releasabl