ArticleBioconjugate chemistry2019
A Near-IR Fluorescent Dasatinib Derivative That Localizes in Cancer Cells.
Article in Bioconjugate chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 14 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
14 citing papers in PubMed, 28 citations in OpenAlex.
- Quantification of Binding of Small Molecules to Native Kinases by Flow Cytometry Reveals Divergence from Biochemical Affinities.Journal of the American Chemical Society · 2026Article
- In Vitro Evaluation of PARP1 Inhibitor Olaparib-Cyanine Dye Conjugate for the Treatment of Glioblastoma.ChemMedChem · 2026Article
- Cyanines Substituted on the Polymethine Chain: Synthesis, Resulting Properties, and Application Use Cases.ChemPlusChem · 2025Review
- Design Principles and Applications of Fluorescent Kinase Inhibitors for Simultaneous Cancer Bioimaging and Therapy.Cancers · 2024Review
- Small molecules and conjugates as theranostic agents.RSC chemical biology · 2023Review
- Development of Iodinated Indocyanine Green Analogs as a Strategy for Targeted Therapy of Liver Cancer.ACS medicinal chemistry letters · 2023Article
- Mitochondrion-Targeted NIR Therapeutic Agent Suppresses Melanoma by Inducing Apoptosis and Cell Cycle Arrest via E2F/Cyclin/CDK Pathway.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Fluorescent PARP Inhibitors Applied To Intracranial Glioblastoma: Accumulation and Persistence In Vivo.ACS medicinal chemistry letters · 2022Article
- Synthesis and Investigation of Derivatives of 1,8-Naphthalimide with a Red Emission via an Aromatic Nucleophilic Substitution Reaction.Journal of fluorescence · 2022Article
- Fluorescent kinase inhibitors as probes in cancer.Chemical Society reviews · 2021Review
- Cyanine conjugates in cancer theranostics.Bioactive materials · 2021Review
- The Use of Heptamethine Cyanine Dyes as Drug-Conjugate Systems in the Treatment of Primary and Metastatic Brain Tumors.Frontiers in oncology · 2021Review
- Recent advances in construction of small molecule-based fluorophore-drug conjugates.Journal of pharmaceutical analysis · 2020Review
- TrkC-Targeted Kinase Inhibitors And PROTACs.Molecular pharmaceutics · 2019Article
Corrections and comments
- Erratum issued
Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Kinase inhibitors (KIs) have had a huge impact on clinical treatment of various cancers, but they are far from perfect medicines. In particular, their efficacies are limited to certain cancer types and, in many cases, provide only temporary remission. This paper explores the possibility of covalently binding a fluorophore for in vivo optical imaging to the KI dasatinib where the particular fluorophore chosen for this study, a heptamethine cyanine (Cy) derivative, tends to accumulate in tumors. Thus, we hypothesized that the dasatinib-fluorophore conjugate might target tumor cells more effectively than the parent KI, give enhanced suppression of viability, and simultaneously serve as a probe for optical imaging. As far as we are aware, the dasatinib conjugate (1) is the first reported to contain this KI and a probe for near-IR imaging, and it is certainly the first conjugate of a tumor-targeting near-IR dye and a KI of any kind. Conjugate 1 suppressed the viability of liver cancer cells (HepG2) more effectively than dasatinib at the same concentration. In scratch assays, 1 prevented regrowth of the tumor cells. Conjugate 1 is cell permeable, and confocal imaging indicates the fluorescence of those cells is concentrated in the mitochondria than lysosomes. In general, this study suggests there is untapped potential for conjugates of KIs with tumor-targeting near-IR dyes in the development of theranostics for optical imaging and treatment of cancer.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.