2. Cell Cycle/DNA Damage
    Antibody-drug Conjugate/ADC Related
    Anti-infection
    Apoptosis
  3. DNA Alkylator/Crosslinker
    ADC Cytotoxin
    Bacterial
    Apoptosis
    Antibiotic
  4. Calicheamicin

Calicheamicin  (Synonyms: Calicheamicin γ1)

Cat. No.: HY-19609 Purity: 98.19%
COA Handling Instructions

Calicheamicin, an antitumor antibiotic, is a cytotoxic agent that causes double-strand DNA breaks. Calicheamicin is a DNA synthesis inhibitor.

For research use only. We do not sell to patients.

Calicheamicin Chemical Structure

Calicheamicin Chemical Structure

CAS No. : 108212-75-5

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1 mg USD 280 In-stock
5 mg USD 690 In-stock
10 mg USD 1100 In-stock
25 mg USD 2200 In-stock
50 mg USD 3500 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Calicheamicin:

Top Publications Citing Use of Products

    Calicheamicin purchased from MCE. Usage Cited in: FASEB J. 2018 Jun 6:fj201800092R.  [Abstract]

    The distribution of PARP-1 is compared in the 4 fractions after Neocarzinostatin (NCS) or Calicheamicin (Cali) treatment in Ku70-deficient and Ku70-normal MDA-MB-231 and BT-549 cells.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Calicheamicin, an antitumor antibiotic, is a cytotoxic agent that causes double-strand DNA breaks. Calicheamicin is a DNA synthesis inhibitor[1].

    IC50 & Target

    Calicheamicins

     

    In Vitro

    PF-06647263 (anti-EFNA4-ADC) is generated via conjugation of 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 elicits antigen- and concentration-dependent cytotoxicity, as exposure to PF-06647263 for 96 hours results in cell death (EC50= appr 1 ng/mL)[1]. CMC-544, consisting of a humanized CD22 Ab linked to calicheamicin, is effective in pediatric primary B-cell precursor acute lymphoblastic leukemia (BCP-ALL) cells in vitro. CMC-544 induces cell death in various ALL cell lines in a dose- and time-dependent way, with IC50 values ranging from 0.15 to 4.9 ng/mL. CMC-544 (10 ng/mL) is effective and specific in primary BCP-ALL cells[2]. In CMC-544-treated cells, the level of CD22 has decreased relative to that on G5/44-treated cells and continued to decrease[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    In Vivo

    An ADC comprising a humanized anti-EFNA4 monoclonal antibody conjugated to the DNA-damaging agent calicheamicin achieves sustained tumor regressions in both TNBC and ovarian cancer PDX in vivo. PF-06647263 (0.27, 0.36 mg/kg) results in significant tumor regressions in TNBC xenografts[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    1368.35

    Appearance

    Solid

    Formula

    C55H74IN3O21S4
    CAS No.
    SMILES
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (18.27 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 0.7308 mL 3.6540 mL 7.3081 mL
    5 mM 0.1462 mL 0.7308 mL 1.4616 mL
    10 mM 0.0731 mL 0.3654 mL 0.7308 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 3 mg/mL (2.19 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (1.83 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.5 mg/mL (1.83 mM); Suspended solution; Need ultrasonic

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 98.28%

    COA (261 KB) HNMR (381 KB) LCMS (83 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [3]

    The enhancement of the CDC effect is studied in a similar way in the presence of CMC-544 or G5/44. Specifically, after cells are incubated with or without CMC-544 (5 ng/mL calichemicin DMH) or G5/44 at 37°C for 2 h, they are washed three times to remove unbound antibodies. The viability of cells before incubation with CMC-544 is 99.8%.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Cohorts of tumor-bearing mice (140-180 mm3) are randomized into study groups of 6 to 10 based on the number of available mice. The IDBS electronic notebook statistical package, Biobook, is used for automated animal randomization. Animals are dosed by intraperitoneal injection (or intravenously for 144580) twice a week for 4 cycles with ADC, or once a week for 2 cycles with 1.5 mg/kg NSC 123127 for breast PDX tumors or 5 mg/kg NSC 119875 for ovarian PDX. Study groups are followed until either individual mice or entire cohort measurements reach 1,200 mm3, at which point sacrifice is indicated. Tumor regression is defined as a reduction in mean tumor volume after dosing. In cases where tumors regress, time to progression (TTP) is determined to be the number of days between the first dose and the time at which mean tumor volume significantly increase (regrow) after regression.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    Calicheamicin108212-75-5Calicheamicin γ1Calicheamicin γ 1Calicheamicin γ-1DNA Alkylator/CrosslinkerADC CytotoxinBacterialApoptosisAntibioticADC PayloadInhibitorinhibitorinhibit

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