1. Cell Cycle/DNA Damage
    Antibody-drug Conjugate/ADC Related
  2. DNA Alkylator/Crosslinker
    ADC Cytotoxin

Calicheamicin (Synonyms: Calicheamicin γ1)

Cat. No.: HY-19609 Purity: 98.44%
Data Sheet SDS Handling Instructions

Calicheamicin is a potent DNA-damaging cytotoxic agent.

For research use only. We do not sell to patients.
Calicheamicin Chemical Structure

Calicheamicin Chemical Structure

CAS No. : 108212-75-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO $2258 In-stock
1 mg $400 In-stock
5 mg $850 In-stock
10 mg $1500 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Other Forms of Calicheamicin:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Calicheamicin is a potent DNA-damaging cytotoxic agent.

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].

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].

References
Preparing Stock Solutions
Concentration Volume 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.
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%. After the cells are re-incubated in CMC-544- and rituximab-free medium at 37°C for 0-48 h, CDC is analyzed. 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 doxorubicin for breast PDX tumors or 5 mg/kg Cisplatin 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
Molecular Weight

1368.35

Formula

C₅₅H₇₄IN₃O₂₁S₄

CAS No.

108212-75-5

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 98.44%

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Product Name:
Calicheamicin
Cat. No.:
HY-19609
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