Cancer markers and methods of use
Breast cancer, technology for use in antibody and/or immunogenic conjugate compositions, vaccines, treatment or detection of hyperproliferative diseases and/or conditions, carbohydrase inhibitor compounds and compositions thereof, selection of cancer stem cells In the field of labeling, it can solve the problem of insufficient enrichment of CSC
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[0514] Preparation of antibody-drug conjugates
[0515] In the antibody-drug conjugate (ADC) of the present invention, the antibody (Ab) is bound to one or more drug moieties (D) via a linker (L), eg, about 1 to about 20 drug moieties per antibody. ADCs of formula I can be prepared by several routes using organic chemistry reactions, conditions and reagents known to those skilled in the art, including: (1) reaction of the nucleophilic group of the antibody with a divalent linker reagent, via co- A valent bond forms Ab-L, which subsequently reacts with the drug moiety D; and (2) the nucleophilic group of the drug moiety reacts with a divalent linker reagent to form D-L via a covalent bond, which subsequently reacts with the nucleophilic group of the antibody reaction. Additional methods of making ADCs are described herein.
[0516] Ab-(L-D)pI
[0517] A connector can consist of one or more connector components. Exemplary linker components include 6-maleimidocaproyl ("MC"), ...
example 1
[0584] Example 1: Exemplary Synthesis of SSEA3 Analogs
[0585] Process 1.
[0586] Compounds Gb4 analogs, ATP, UTP, galactose analogs, phosphoenolpyruvate, magnesium chloride and the enzymes galactokinase (GalK), UDP sugar pyrophosphorylase (AtUSP), β-1,3-galactosyl Transferase (LgtD), pyruvate kinase (PK) and inorganic pyrophosphatase (PPA) were combined in solution, the reaction was initiated at room temperature with pH controlled at 7.0, and the reaction was monitored by TLC until no more product was observed. After the reaction was complete, the protein in the reaction mixture was removed by heating for 30 minutes, followed by centrifugation and filtration with a 0.22 μΜ filter. The filtrate was then purified by C-18 gel chromatography. Fractions were collected and monitored by TLC.
example 2
[0587] Example 2: Exemplary Synthesis of SSEA4 Analogs
[0588] Method 1: Chemical synthesis of SSEA4-Gc
[0589] Compounds 1-6 were prepared by methods reported in literature. Powdered molecular sieves (4A, 0.5 g) were added to acceptor 3 (93 mg, 0.045 mmol) and imide ester 6 (76 mg, 0.068 mmol) in 6 mL of dichloromethane (CH 2 Cl 2 ) in the solution. The mixture was stirred at room temperature for 2 hours. After cooling to -10°C, TMSOTf (5 μL, 0.03 mmol) was added, and the mixture was stirred overnight at 5°C (cold room). The reaction mixture was quenched by adding triethylamine (0.5 mL), washed with CH 2 Cl 2 Dilute and filter through a pad of celite. The filtrate was washed with saturated sodium bicarbonate (NaHCO 3 ) aqueous solution, washed with sodium sulfate (Na 2 SO 4 ) was removed from water, filtered and concentrated. The residue was purified by flash silica gel chromatography (50-100% EtOAc in hexanes) to afford the hexasaccharide 7 mixed with impurities...
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