Calicheamicins are a class of enediyne antitumor antibiotics derived from the bacterium Micromonospora echinospora, The main component is calicheamicin γ1. It has strong anti-Gram-positive bacteria activity and anti-tumor effect.
Structure of 108212-75-5
* For research and manufacturing use only. We do not sell to patients.
Size | Price | Stock | Quantity |
---|---|---|---|
1 mg | $376 | In stock | |
5 mg | $839 | In stock | |
10 mg | $1498 | In stock |
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Capabilities & Facilities
Calicheamicin is a potent enediyne antibiotic and a highly cytotoxic ADC payload widely used in antibody-drug conjugates for targeted cancer therapy. Its cytotoxic mechanism involves sequence-specific binding to the minor groove of DNA, followed by oxidative DNA strand cleavage through enediyne-mediated activation. This leads to DNA double-strand breaks, cell cycle arrest, and induction of apoptosis in proliferating tumor cells. Calicheamicin’s structure allows covalent conjugation to monoclonal antibodies via cleavable or non-cleavable linkers, enabling precise intracellular delivery in ADC applications while maintaining systemic stability.
Within antibody-drug conjugates, Calicheamicin is attached to antibodies using linker chemistries optimized for plasma stability and controlled intracellular release. The ADC remains inactive in circulation, minimizing off-target cytotoxicity. Upon receptor-mediated internalization into antigen-expressing tumor cells, enzymatic or chemical cleavage of the linker liberates the active Calicheamicin payload. Once released, it binds to the DNA minor groove and induces DNA strand cleavage, leading to apoptosis. This targeted mechanism ensures that cytotoxic effects are confined to tumor cells, supporting precise tumor-targeted therapy in ADC constructs.
Applications of Calicheamicin include incorporation into ADCs targeting hematologic malignancies and solid tumors with specific antigen expression. Its chemical compatibility with diverse linker systems allows optimization of conjugation efficiency, intracellular release kinetics, and pharmacokinetic profiles. Preclinical and clinical studies demonstrate potent cytotoxicity in antigen-expressing tumor cells. Calicheamicin supports the development of ADCs with defined DNA-damaging mechanisms, providing mechanistically precise induction of apoptosis and tumor cell elimination, facilitating rational design and evaluation of antibody-drug conjugates in oncology applications.
Catalog | Product Name | CAS | Inquiry |
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BADC-00723 | N-Acetyl-Calicheamicin | 108212-76-6 |
What is Calicheamicin?
Calicheamicin is a potent enediyne antitumor antibiotic used as a cytotoxic payload in ADCs. It binds to the DNA minor groove and induces double-strand breaks, leading to rapid apoptosis of targeted cells.
24/8/2019
Could you explain how Calicheamicin is applied in ADCs?
Calicheamicin is conjugated to antibodies via cleavable or non-cleavable linkers to selectively deliver cytotoxic effects to antigen-expressing tumor cells, enhancing ADC efficacy while limiting systemic toxicity.
12/3/2017
We would like to know which linkers are suitable for Calicheamicin.
Calicheamicin is compatible with disulfide and other cleavable linkers, allowing controlled drug release in target cells. Non-cleavable linkers can also be used depending on desired pharmacokinetics and stability.
22/12/2018
Good morning! Could you let me know if BOC Sciences can provide Calicheamicin ADC services?
BOC Sciences offers Calicheamicin ADC development services including payload conjugation, linker optimization, and analytical characterization, enabling tailored ADC constructs for preclinical research.
15/8/2017
Good morning! What safety measures should be followed when handling Calicheamicin?
Calicheamicin is extremely cytotoxic and requires stringent handling protocols, including use of PPE, biosafety cabinets, and strict laboratory procedures to ensure safe manipulation during research.
4/12/2020
— Dr. Peter Hall, Senior Scientist (USA)
Calicheamicin delivered by BOC Sciences exhibited exceptional purity, supporting precise conjugation protocols.
22/12/2018
— Dr. Richard Miller, Oncology Researcher (USA)
Calicheamicin provided by BOC Sciences was of outstanding quality, enabling precise and reproducible conjugation studies.
4/12/2020
— Ms. Julia Schneider, Senior Scientist (Germany)
Fast and reliable supply of Calicheamicin with complete analytical data allowed us to accelerate our ADC research.
15/8/2017
— Dr. Andrew Clarke, Project Lead (UK)
Consistency in Calicheamicin batches has been key to successful linker-payload development in our projects.
24/8/2019
— Mr. François Dubois, Medicinal Chemist (France)
BOC Sciences’ support regarding Calicheamicin technical questions was prompt and professional.
— Dr. Emilia Johansson, Biotech Scientist (Sweden)
Reliable sourcing of Calicheamicin allowed us to maintain high reproducibility and advance our preclinical studies.
12/3/2017
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