Calicheamicin

SKU: orb1308500

Description

Calicheamicin γ1 is a potent antitumor antibiotic that inhibits DNA synthesis by inducing cytotoxic double-strand DNA breaks. It is widely used as a payload in antibody-drug conjugates (ADCs) for targeted cancer therapy and serves as a critical tool in oncology research for studying DNA damage mechanisms in vitro and in vivo.

Research Area

Cell Biology, Infectious Disease & Virology, Molecular Biology

Key Properties

• CAS Number: 108212-75-5
• MW: 1368.35
• Formula: C₅₅H₇₄IN₃O₂₁S₄
• SMILES: [H][C@@]1(C[C@H](OC)[C@H](CO1)NCC)O[C@@H]1[C@@H](O)[C@H](NO[C@H]2C[C@H](O)[C@H](SC(=O)c3c(C)c(I)c(O[C@@H]4O[C@@H](C)[C@H](O)[C@@H](OC)[C@H]4O)c(OC)c3OC)[C@@H](C)O2)[C@@H](C)O[C@@]1([H])O[C@H]1C#C\C=C/C#C[C@]2(O)CC(=O)C(NC(=O)OC)=C1\C2=C\CSSSC
• Target: ADC Cytotoxin
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (2.92 mM);DMSO:100 mg/mL (73.08 mM)

Bioactivity

• In Vitro:
  PF-06647263 (anti-EFNA4-ADC) is generated by conjugating hE22 lysine residues to the AcButDMH-N-Ac-calicheamicin-γ1 linker-payload, with an average drug-to-antibody ratio (DAR) of 4.6. PF-06647263 induces antigen- and concentration-dependent cytotoxicity, causing cell death after 96 hours of exposure (EC50: ~1 ng/mL) .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Calicheamicin, Calicheamicin gamma1, Calicheamicin r1, Calicheamicin γ 1, Calicheamicin γ1, Calicheamicin γ-1, Calicheamicins, ADCCytotoxin, ADC Cytotoxin

Compound Identifiers

PubChem CID

101617325