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Calicheamicin Tumor Antibiotic Cytotoxic Agent

Calicheamicin Tumor Antibiotic Cytotoxic Agent

English name：Calicheamicin
CAS number：108212-75-5
Another name:
calicheamicin gamma(1)I; Benzenecarbothioic acid, 4-((6-deoxy-3-o-methyl-alpha-L-mannopyranosyl)oxy)-3-iodo-5,6-dimethoxy-2-methyl-, 4''-ester with methyl (8-((4,6-dideoxy-2-o-(2,4-dideoxy-4-(ethylamino)-3-o-methyl-alpha-L-threo-pentapyranosyl)-4-(((2,6-dideoxy-4-thio-beta-D-ribo-hexopyranosyl)oxy)amino)-beta-D-glucopyranosyl)oxy)-1-hydroxy-13-(2-(methyltrithio)ethylidene)-11-oxobicyclo(7.3.1)trideca-4,9-diene-2,6-diyn-10-yl)carbamate, (1R-(1R*,4Z,8S*,13E))-; Calichemicin gamma1; Carbamic acid, ((1R,4Z,8S,13E)-8-((4,6-dideoxy-4-(((2,6-dideoxy-4-S-(4-((6-deoxy-3-o-methyl-alpha-L-mannopyranopyranosyl)oxy)-3-iodo-5,6-dimethoxy-2-methylbenzoyl)-4-thio-beta-D-ribo-hexopyranosyl)oxy)amino)-2-o-(2,4-dideoxy-4-(ethylamino)-3-o-methyl-alpha-L-threo-pentopyranosyl)-beta-D-glucopyranosyl)oxy)-1-hydroxy-13-(2-(methyltrithio)ethylidene)-11-oxobicyclo(7.3.1)trideca-4,9-diene-2,6-diyn-10-yl)-, methyl ester; Calicheamicin γ1; LL-E 33288 gamma1-I; calicheamicin gamma; Calicheamicin γ1 purity>95
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Products Description

 

English name：Calicheamicin

CAS number：108212-75-5

Molecular formula: C55H74IN3O21S4

Molecular weight: 1,368.34

EINECS No:

Related categories: API [for scientific research only]; pharmaceutical API; scientific research active drug series; API; API and intermediates; reagents; others; chemical reagents; ADC; Pharmaceutical

The Mol file: 108212-75-5.mol

 

Molecular structure:

1 -

 

Calithromycin properties

Specific rotation: D26-124 (c = 0.98%, EtOH)

Density: 1.57 ± 0.1 g/cm3 (Predicted)

Storage conditions: Store at-20 C

Solubility: DMSO: 100 mg/mL (73.08 mM); water: <0.1 mg / mL (insoluble)

Form: solid

Aciity coefficient (pK a): 7.13 ± 0.60 (Predicted)

Color: White to yellow

 

Use and synthesis method of Calicimamycin

 

Brief introduction

calicheamicins (CLM) is an enediyne anti-tumor antibiotic isolated from the fermentation broth of rare small monosporum.

 

Mechanism of action

The bioactive concentration of carchithromycin <1 PgmL-1 had extremely potent killing effects in leukemia such as lymphocytic leukaemia P388 and L1210 cells as well as solid tumors such as colon cancer 26 and melanoma B-16 cells. The biological activity of cazithromycin mainly by combining cellular DNA with the Chemicalbook minor groove, directly break cell DNA, further induce tumor cell apoptosis, at the same time, cazithromycin has nonspecific damage effect on cellular RNA, Mylotarg with CD33 monoclonal antibody conjugate is the first approved by the FDA for tumor treatment, has been used in clinical practice.

 

Use

Cchithromycin is a potent cytotoxic agent that can cause DNA double strand breaks.

 

Toxicity

Cachithromycin is highly toxic and is one of hundreds of metabolites produced by soil bacteria.

 

Bioactivity

Calicheamicin Is a tumor antibiotic and also a potent cytotoxic agent, causing DNA double-strand breaks. Calicheamicin Inhibition of DNA synthesis.

 

Target spot

Calicheamicins

 

In vitro study

PF-06647263(anti-EFNA4-ADC)isgeneratedviaconjugationofhE22lysineresiduestotheAcButDMH-N-Ac-calicheamicin-γ1linker-payloadwithanaveragedrug-to-antibodyratio(DAR)of4.6.PF-06647263elicitsantigen-andconcentration-dependentcytotoxicity,asexposuretoPF-06647263for96hoursresultsincelldeath(EC50=appr1ng/mL).CMC-544,consistingofahumanizedCD22Ablinkedtocalicheamicin,iseffeChemicalbookctiveinpediatricprimaryB-cellprecursoracutelymphoblasticleukemia(BCP-ALL)cellsinvitro.CMC-544inducescelldeathinvariousALLcelllinesinadose-andtime-dependentway,withIC50valuesrangingfrom0.15to4.9ng/mL.CMC-544(10ng/mL)iseffectiveandspecificinprimaryBCP-ALLcells.InCMC-544-treatedcells,thelevelofCD22hasdecreasedrelativetothatonG5/44-treatedcellsandcontinuedtodecrease.

 

In vivo research

AnADCcomprisingahumanizedanti-EFNA4monoclonalantibodyconjugatedtotheDNA-damagingagentcalicheamicinachievessustainedtumorregChemicalbookressionsinbothTNBCandovariancancerPDXinvivo.PF-06647263(0.27,0.36mg/kg)resultsinsignificanttumorregressionsinTNBCxenografts.

 

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