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Calicheamicin

Catalog No. T14858 CAS 108212-75-5

Synonyms: Calicheamicin γ1

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

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Calicheamicin, CAS 108212-75-5

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Calicheamicin is an antitumor antibiotic and is a DNA synthesis inhibitor. It also is a cytotoxic agent that causes double-strand DNA breaks.
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: ~1 ng/mL) [1].
In vivo	PF-06647263 (0.27, 0.36 mg/kg) results in significant tumor regressions in TNBC xenografts. 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 [1].

Synonyms	Calicheamicin γ1
Molecular Weight	1368.35
Formula	C55H74IN3O21S4
CAS No.	108212-75-5

Storage

贵重物品 store at -20

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 100 mg/mL (73.08 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Damelin M, et al. Anti-EFNA4 Calicheamicin Conjugates Effectively Target Triple-Negative Breast and Ovarian Tumor-Initiating Cells to Result in Sustained Tumor Regressions. Clin Cancer Res. 2015 Sep 15;21(18):4165-73 2. de Vries JF, et al. The novel calicheamicin-conjugated CD22 antibody inotuzumab ozogamicin (CMC-544) effectively kills primary pediatric acute lymphoblastic leukemia cells. Leukemia. 2012 Feb;26(2):255-64 3. Takeshita A, et al. CMC-544 (inotuzumab ozogamicin), an anti-CD22 immuno-conjugate of calicheamicin, alters the levels of target molecules of malignant B-cells. Leukemia. 2009 Jul;23(7):1329-36.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Calicheamicin 108212-75-5 Others ADC Cytotoxin Bacterial Inhibitor Apoptosis inhibit ADC Payload Calicheamicin γ 1 Calicheamicin γ1 DNA Alkylator/Crosslinker Calicheamicin γ-1 Antibiotic inhibitor

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