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Citotoksično sredstvo protiv kalikeamicina

Citotoksično sredstvo protiv kalikeamicina

Engleski naziv: kalicheamicin
CAS broj: 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
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Opis proizvoda

 

Englesko ime: Kalicheamicin

CAS broj: 108212-75-5

Molekularna formula: C55H74IN3O21S4

Molekularna masa: 1.368,34

EINECS NE:

Povezane kategorije: API [samo za znanstvena istraživanja]; Farmaceutski API; Znanstvena istraživačka aktivna serija droga; API; API i intermedijari; reagensi; drugi; Kemijski reagensi; ADC; Farmaceutski

Mol datoteka: 108212-75-5. Mol

 

Molekularna struktura:

1 -

 

Svojstva kalitromicina

Specifična rotacija: D 26-124 (C=0. 98%, EtOH)

Gustoća: 1,57 ± 0. 1 g/cm3 (predviđeno)

Uvjeti za pohranu: pohranite na -20 c

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

Obrazac: Čvrsta

Koeficijent za vrijeme (PK A): 7,13 ± 0. 60 (predviđeno)

Boja: bijela do žuta

 

Metoda upotrebe i sinteze kalicimamicina

 

Kratak uvod

Calicheamicinis (CLM) je enediyne anti-tumorski antibiotik izoliran iz fermentacijske juhe rijetkog malog monosporuma.

 

Mehanizam djelovanja

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.

 

Koristiti

Cchitromicin je moćno citotoksično sredstvo koje može uzrokovati proboj dvostrukih niti DNK.

 

Toksičnost

Kahitromicin je vrlo toksičan i jedan je od stotina metabolita proizvedenih bakterijama tla.

 

Bioaktivnost

Kalicheamicin je tumorski antibiotik i također moćno citotoksično sredstvo, uzrokujući DNK dvostruki lomovi. Inhibicija sinteze DNA kalikeamicicina.

 

Ciljano mjesto

Kalikemicini

 

In vitro studija

Pf {{{0}} (anti-efna 4- adc) IsgeneratedviaConjugationOfHe22lysinerisiduestotheacbutdmh-n-ac -calicheamicin - 1 veznik-payload withanaVanageRug-to-AntiBidyratio (dar) od4.6.pf -06647263 elicitsa ntigen-i-ikontracija-ovisnacytotoksičnost, asexpoSuretopf -06647263 For96HourSresultSincellDeath (EC 50= APPR1NG/ML) .CMC {-544, COLENGINGOFAHICEDCDICDCD BoodEdRimPrimaryb-CellPrecursoracturyMphoblasticleukemia (BCP-all) Cellvitro.cmc -544 inducescellDathinVariousAllCellLineSiNadodeSinadose-Oviseway OM0.15TO4.9NG/ML.CMC -544 (10ng/ml) ISEFFECTIVEANDSPECIFIFIFINPIMARYBCP-AllCells.IncMC -544- TREA tedcells, thelevelofcd22HasDecroudeLelativetothatong5/{44- trethedCellSandContinuedTodecrease.

 

Istraživanje in vivo

Anadccomprisisahumanidanti-efna4monoclonantiBonjugidatedTotheDNA-damagentcalicheamicicicIchinachieveSustainedTumorregchemical KOLKESSIONSINBOTHTNBCANDOVARIARCANCERPDXINVIVO.PF -06647263 (0. 27, 0. 36Mg/kg) Rezultati znamenitanttumorresionsionsIntnnbcxenografts.

 

Popularni tagovi: Kalicheamicin tumorski antibiotsko citotoksično sredstvo, Kina Calicheamicin tumorski antibiotsko citotoksično sredstvo, 130288-24-3, 146478-72-0, 57103-68-1, 646502-53-6, 77668-69-0, MMAF OME inhibitori