CALICHEAMICIN TUMOVNI KITOTOXIČNI SMETNI

Angleško ime: Calicheamicin
Številka CAS: 108212-75-5
Drugo ime:
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

Pošlji povpraševanje

Opis izdelkov

Angleško ime: Calicheamicin

Številka CAS: 108212-75-5

Molekularna formula: C55H74IN3O21S4

Molekularna teža: 1,368,34

Einecs št:

Povezane kategorije: API [samo za znanstvene raziskave]; Farmacevtski API; Znanstvene raziskave aktivne serije zdravil; API; API in intermediati; reagenti; drugi; kemični reagenti; ADC; Farmacevtska

Datoteka mol: 108212-75-5. Mol

Molekularna struktura:

1 -

Lastnosti kalitromicina

Specifično vrtenje: D 26-124 (C=0. 98%, etoh)

Gostota: 1,57 ± 0. 1 g/cm3 (predvideno)

Pogoji shranjevanja: Shranjujte na -20 c

Topnost: DMSO: 100 mg/ml (73,08 mm); voda:<0.1 mg / mL (insoluble)

Oblika: trdna

Koeficient aciity (pk a): 7,13 ± 0. 60 (napovedano)

Barva: bela do rumena

Uporaba in sinteza metoda kalicimamicina

Kratek uvod

Kalicheamicini (CLM) so enediinski anti-tumorski antibiotik, izoliran iz fermentacijske juhe redkega majhnega monospoma.

Mehanizem delovanja

Bioaktivna koncentracija karhitromicina<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.

Uporaba

Cchitromicin je močno citotoksično sredstvo, ki lahko povzroči prelome dvojnega pramena DNK.

Strupenost

Kahitromicin je zelo strupen in je eden od sto presnovkov, ki jih proizvajajo talne bakterije.

Bioaktivnost

Calicheamicin je tumorski antibiotik in tudi močan citotoksični sredstvo, ki povzroča dvojne prelome DNK. Kalicheamicin inhibicija sinteze DNK.

Ciljno mesto

Kalicheamicini

Študija in vitro

Pf {{0}} (anti-efna 4- adc) isgeneratedviaConjugationOfHe22lysineResidueStheacbutdmh-n-ac -calicheamicin - 1 linker-payloadWithanaveragedRug-to-Antibodyratio (DAR) OF4.6.pf -06647263 elicitsa ntigen-andconcentration-dependentcytotoxicity,asexposuretoPF-06647263for96hoursresultsincelldeath(EC50=appr1ng/mL).CMC-544,consistingofahumanizedCD22Ablinkedtocalicheamicin,iseffeChemical BookctiveInpediatricPrimaryB-cellprecursurteRacultemphobullasticleukemia (BCP-ALL) CELLSINVITRO.CMC -544 inducescellDeathinvarioulcellLinesinAdose-and-and odvisnih poti, Wic50ValuesRangingfr OM0.15TO4.9NG/ML.CMC -544 (10NG/ml) ISEFFECTIVEANDSPECIFICICICICICICINPRIMARIBCP-ALLCELLS.INCMC -544- Trea TedCells, theLevelofcd22hasDecRedreLativetothatong5/44- obdelanecellSantContinuedToDecrease.

Raziskave in vivo

AnadcComprisisingAhumanizent-efna4moclonalantibodyconjugingtothedna-damagingcalichamicinachievessatedtumorreghemični boocresionBothtnbcandovarianCancerpdxinvivo.pf -06647263 (0.

Priljubljena oznake: Citotoksično sredstvo za kalicheamicin tumorski antibiotik, kitajska dobavitelji citotoksičnega zdravila China Calicheamicin tumor