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MC-Sq-Cit-PAB-Gefitinib is a drug-linker conjugate for ADC with potent antitumor activity by using Gefitinib (an EGFR tyrosine kinase inhibitor), linked via the ADC linker MC-Sq-Cit-PAB.
| Catalog Number | Size | Price | Quantity | |
|---|---|---|---|---|
| BADC-00623 | -- | $-- | Inquiry |
MC-Sq-Cit-PAB-Gefitinib is a conjugate that combines the potent anticancer drug gefitinib with a targeted delivery system to enhance its specificity and efficacy in cancer therapy. Gefitinib is an epidermal growth factor receptor (EGFR) inhibitor commonly used in the treatment of non-small cell lung cancer (NSCLC) and other EGFR-driven cancers. When conjugated to a peptide or antibody linker, such as the MC-Sq-Cit-PAB component, gefitinib's delivery is more targeted, reducing systemic side effects and improving therapeutic outcomes. This conjugate represents a promising approach for enhancing the precision of cancer treatments.
One of the primary applications of MC-Sq-Cit-PAB-Gefitinib is in the development of antibody-drug conjugates (ADCs) for targeted cancer therapy. By linking gefitinib to a peptide or antibody that selectively binds to specific cancer cell markers, this conjugate ensures that the drug is delivered directly to the tumor site. This increases the concentration of gefitinib at the tumor while reducing exposure to healthy tissues. The targeted delivery system improves the overall efficacy of gefitinib by overcoming issues like drug resistance and non-selective cytotoxicity, which are common with traditional chemotherapy.
MC-Sq-Cit-PAB-Gefitinib is also applied in improving the pharmacokinetics of gefitinib. Traditional oral administration of gefitinib may result in suboptimal bioavailability or systemic toxicity. However, by conjugating gefitinib to a specialized carrier molecule such as MC-Sq-Cit-PAB, the drug's stability, solubility, and bioavailability are enhanced. This conjugation strategy also enables controlled release at the tumor site, optimizing the therapeutic dose delivered to cancer cells while minimizing side effects. Researchers are exploring MC-Sq-Cit-PAB-Gefitinib in preclinical models to refine its pharmacokinetic profile and extend its therapeutic potential.
Another important application of MC-Sq-Cit-PAB-Gefitinib is in overcoming drug resistance mechanisms. Many cancers develop resistance to gefitinib and other EGFR inhibitors through various mechanisms, such as mutations in the EGFR gene. The targeted delivery of gefitinib via MC-Sq-Cit-PAB can potentially bypass some of these resistance pathways by ensuring that the drug is specifically delivered to the tumor cells, where it can exert its therapeutic effects. This approach could offer a solution for patients with resistant cancer strains, expanding the range of patients who can benefit from EGFR-targeted therapies.
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BOC Sciences offers comprehensive services for ADC manufacturing, including antibody modification, linker chemistry, payload conjugation, and formulation development. In particular, our payload-linker customization service offers a convenient and fast raw material channel for many ADC researchers.
BOC Sciences provides one-stop site-specific conjugation services for amino acids, glycans, unnatural amino acids, and short peptide tags. In addition, cysteine conjugation, lysine conjugation, enzymatic conjugation, thio-engineered antibody can also be obtained quickly.
BOC Sciences offers a full range of linkers, including peptide linkers, PEG linkers, click chemistry, PROTAC linkers, non-cleavable linkers, etc. We also provide custom development services for chemically labile linkers and enzymatically cleavable linkers.
