Daniel Custar
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A Novel Concept for Cleavable Linkers Applicable to Conjugation Chemistry – Design, Synthesis and Characterization Open
Linkers with disulfide bonds are the only cleavable linkers that utilize physiological thiol gradients as a trigger to initiate the intracellular drug release cascade. Herein, we present a novel concept exploiting the thiol gradient phenom…
Supplementary Data from Development of a Novel DNA Mono-alkylator Platform for Antibody–Drug Conjugates Open
Supplementary Materials and Methods including Assays and Synthetic Procedures
Table S8 from Development of a Novel DNA Mono-alkylator Platform for Antibody–Drug Conjugates Open
Table shows Tabulated cell growth inhibition data for NCI-N87 and MDA-MB231 cells in monoculture and coculture when treated with ADCs T-16, T-17, and T-18
Figure S4 from Development of a Novel DNA Mono-alkylator Platform for Antibody–Drug Conjugates Open
Figure shows In vitro activity of NaPi2b ADCs X-BG and X-19 and payload 4 in the OVCAR3 cell line
Table S7 from Development of a Novel DNA Mono-alkylator Platform for Antibody–Drug Conjugates Open
Table shows Cytotoxicity comparisons between Biaryl PBD ADCs vs DGN549 ADCs
Table S3 from Development of a Novel DNA Mono-alkylator Platform for Antibody–Drug Conjugates Open
Table shows Payload in vitro potency in various cell lines.
Figure S6 from Development of a Novel DNA Mono-alkylator Platform for Antibody–Drug Conjugates Open
Figure shows comet assay results
Supplementary Data from Development of a Novel DNA Mono-alkylator Platform for Antibody–Drug Conjugates Open
Supplementary Materials and Methods including Assays and Synthetic Procedures
Figure S4 from Development of a Novel DNA Mono-alkylator Platform for Antibody–Drug Conjugates Open
Figure shows In vitro activity of NaPi2b ADCs X-BG and X-19 and payload 4 in the OVCAR3 cell line
Table S9 from Development of a Novel DNA Mono-alkylator Platform for Antibody–Drug Conjugates Open
Table shows Cytotoxicity Data for Platforms 18 vs 19
Table S4 from Development of a Novel DNA Mono-alkylator Platform for Antibody–Drug Conjugates Open
Table shows Impact of Tether length and Hydrophilic Modifier on ADC Aggregation and Hydrophobicity
Table S1 from Development of a Novel DNA Mono-alkylator Platform for Antibody–Drug Conjugates Open
Extinction coefficient used to determine DAR for ADCs
Figure S2 from Development of a Novel DNA Mono-alkylator Platform for Antibody–Drug Conjugates Open
Figure shows Structures of Platforms 6, and 8-16
Table S5 from Development of a Novel DNA Mono-alkylator Platform for Antibody–Drug Conjugates Open
Table shows TROP2 receptor quantification on DLD1 and HT29 cells
Figure S8 from Development of a Novel DNA Mono-alkylator Platform for Antibody–Drug Conjugates Open
Figure shows Cytotoxicity of Mesothelin ADCs M-16, M-17, and M-19 in NCI-N87 cell line
Table S1 from Development of a Novel DNA Mono-alkylator Platform for Antibody–Drug Conjugates Open
Extinction coefficient used to determine DAR for ADCs
Figure S1 from Development of a Novel DNA Mono-alkylator Platform for Antibody–Drug Conjugates Open
Structures of PBD Platform 5 and AF-HPA Platform 7 (known as Dolaflexin)
Table S2 from Development of a Novel DNA Mono-alkylator Platform for Antibody–Drug Conjugates Open
MRM Quantification Parameters
Table S7 from Development of a Novel DNA Mono-alkylator Platform for Antibody–Drug Conjugates Open
Table shows Cytotoxicity comparisons between Biaryl PBD ADCs vs DGN549 ADCs
Table S6 from Development of a Novel DNA Mono-alkylator Platform for Antibody–Drug Conjugates Open
Table shows Cytotoxicity comparisons between Biaryl PBD payloads 4 and 20 vs IGN 2
Table S8 from Development of a Novel DNA Mono-alkylator Platform for Antibody–Drug Conjugates Open
Table shows Tabulated cell growth inhibition data for NCI-N87 and MDA-MB231 cells in monoculture and coculture when treated with ADCs T-16, T-17, and T-18
Data from Development of a Novel DNA Mono-alkylator Platform for Antibody–Drug Conjugates Open
Although microtubule inhibitors (MTI) remain a therapeutically valuable payload option for antibody–drug conjugates (ADC), some cancers do not respond to MTI-based ADCs. Efforts to fill this therapeutic gap have led to a recent expansion o…
Table S9 from Development of a Novel DNA Mono-alkylator Platform for Antibody–Drug Conjugates Open
Table shows Cytotoxicity Data for Platforms 18 vs 19
Table S6 from Development of a Novel DNA Mono-alkylator Platform for Antibody–Drug Conjugates Open
Table shows Cytotoxicity comparisons between Biaryl PBD payloads 4 and 20 vs IGN 2
Figure S2 from Development of a Novel DNA Mono-alkylator Platform for Antibody–Drug Conjugates Open
Figure shows Structures of Platforms 6, and 8-16
Figure S3 from Development of a Novel DNA Mono-alkylator Platform for Antibody–Drug Conjugates Open
Figure shows DLD1 xenograft study comparing Biaryl PBD ADCs hR-13 vs hR-DGN549
Data from Development of a Novel DNA Mono-alkylator Platform for Antibody–Drug Conjugates Open
Although microtubule inhibitors (MTI) remain a therapeutically valuable payload option for antibody–drug conjugates (ADC), some cancers do not respond to MTI-based ADCs. Efforts to fill this therapeutic gap have led to a recent expansion o…
Figure S8 from Development of a Novel DNA Mono-alkylator Platform for Antibody–Drug Conjugates Open
Figure shows Cytotoxicity of Mesothelin ADCs M-16, M-17, and M-19 in NCI-N87 cell line
Figure S3 from Development of a Novel DNA Mono-alkylator Platform for Antibody–Drug Conjugates Open
Figure shows DLD1 xenograft study comparing Biaryl PBD ADCs hR-13 vs hR-DGN549
Table S4 from Development of a Novel DNA Mono-alkylator Platform for Antibody–Drug Conjugates Open
Table shows Impact of Tether length and Hydrophilic Modifier on ADC Aggregation and Hydrophobicity