Tyrosine Kinase Inhibitor Development for Brain Tumors
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Tyrosine Kinase Inhibitor Development for Brain Tumors

Tyrosine kinase inhibitors (TKIs) are a class of drugs designed to target tyrosine kinases, and they play a crucial role in cancer therapy by inhibiting the abnormally activated tyrosine kinase signaling pathways that promote tumor cell proliferation and survival. Alfa Cytology is dedicated to advancing tyrosine kinase inhibitors for the treatment of brain tumors. The company offers comprehensive solutions, ranging from target screening to preclinical research, to facilitate the development and translation of novel therapeutic strategies.

Overview of Tyrosine Kinase Inhibitors (TKIs)

Tyrosine kinase inhibitors (TKIs) are targeted therapies used in brain tumors to block abnormal signaling by inhibiting tyrosine kinase activity. Tyrosine kinases regulate cell growth, differentiation, survival, and metabolism, but in tumors like glioblastoma, their activity is often heightened by mutations or overexpression, leading to uncontrolled proliferation. TKIs competitively bind to ATP-binding sites of tyrosine kinases, blocking their phosphorylation and downstream pathways such as PI3K/AKT and RAS/MAPK, thus inhibiting tumor growth, angiogenesis, and metastasis.

Receptor tyrosine kinase and its downstream pathways affected by tyrosine kinase inhibitors.Fig 1. Receptor tyrosine kinase and its downstream pathways affected by tyrosine kinase inhibitors. (SHYAM SUNDER S, et al., 2023)

Classification of Tyrosine Kinase Inhibitors (TKIs)

  • Receptor Tyrosine Kinase Inhibitors

These inhibitors target receptor-type tyrosine kinases (RTKs) located on cell membranes. Key examples include inhibitors for the epidermal growth factor receptor (EGFR) and platelet-derived growth factor receptor (PDGFR).

  • Non-Receptor Tyrosine Kinase Inhibitors

These inhibitors specifically target non-receptor tyrosine kinases within the cell's interior, such as the SRC family kinases and ABL kinases, thereby modulating crucial intracellular signaling pathways and offering promising therapeutic potential.

Pipeline of Tyrosine Kinase Inhibitors Development for Brain Tumors

Company Targets Name Molecule Type Phase
Kazia PI3K / mTOR Inhibitor Paxalisib Small Molecule

Disclaimer: Alfa Cytology focuses on providing preclinical research service. This table is for information exchange purposes only. This table is not a treatment plan recommendation. For guidance on treatment options, please visit a regular hospital.

Our Services

With its cutting-edge molecular biology platform and extensive oncology research expertise, Alfa Cytology is highly equipped to develop tyrosine kinase inhibitors (TKIs) for brain tumors. The company offers a comprehensive suite of services, spanning from target validation to drug optimization. By incorporating high-throughput screening, assessments of blood-brain barrier penetration, and preclinical pharmacodynamic analyses, Alfa Cytology efficiently advances the development of brain tumor-specific TKIs.

Workflow of Tyrosine Kinase Inhibitors Development

Targets Identification

Identify tyrosine kinases abnormally activated in brain tumors through genomic and proteomic analyses. Validate their role in tumor growth and survival using functional studies like CRISPR/Cas9 and RNA interference.

High-Throughput Screening (HTS)

Screen large compound libraries to discover molecules that specifically inhibit the identified tyrosine kinases. Assess their inhibitory effects and cytotoxicity through in vitro assays.

Preclinical Studies

Test the optimized inhibitors in animal models to assess antitumor efficacy. Perform pharmacokinetic and pharmacodynamic studies, and conduct safety and toxicity assessments in compliance with regulatory standards.

Modeling Services for Brain Tumors

Alfa Cytology offers a variety of in vivo and in vitro models for tyrosine kinase inhibitors targeting brain tumors, supporting new drug development and preclinical evaluation.

With cutting-edge molecular biology technology, extensive oncology research expertise, and a specialized platform for assessing blood-brain barrier penetration, Alfa Cytology is well-equipped to deliver efficient and precise development services for TKIs targeting brain tumors. If you have any questions about our services, please don't hesitate to contact us. We are ready to provide detailed technical support and tailor-made solutions to meet your needs.

Reference

  1. SHYAM SUNDER S, SHARMA U C, POKHAREL S. Adverse effects of tyrosine kinase inhibitors in cancer therapy: pathophysiology, mechanisms and clinical management [J]. Signal transduction and targeted therapy, 2023, 8(1): 262.
All of our services and products are intended for preclinical research use only and cannot be used to diagnose, treat or manage patients.