Calicheamicin æxli sýklalyf frumudrepandi lyf

Calicheamicin æxli sýklalyf frumudrepandi lyf

Enska nafnið: Calicheamicin
CAS númer: 108212-75-5
Annað nafn:
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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Vörulýsing

 

Enska nafnið: Calicheamicin

CAS númer: 108212-75-5

Sameindaformúla: C55H74in3O21S4

Mólmassa: 1.368.34

Einecs nr:

Tengdir flokkar: API [eingöngu fyrir vísindarannsóknir]; API lyfja; Vísindarannsóknir virk lyf; API; API og milliefni; hvarfefni; aðrir; efnafræðileg hvarfefni; ADC; Lyfjafyrirtæki

Mol skráin: 108212-75-5. Mol

 

Sameindarbygging:

1 -

 

Calithromycin eiginleikar

Sértæk snúningur: d 26-124 (C=0. 98%, EtOH)

Þéttleiki: 1,57 ± 0. 1 g/cm3 (spáð)

Geymsluskilyrði: Geymið á -20 c

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

Form: Solid

Aciity stuðull (Pk A): 7,13 ± 0. 60 (spáð)

Litur: hvítur til gulur

 

Notkun og myndunaraðferð calicimamycin

 

Stutt kynning

Calicheamicins (CLM) er enediyne sýklalyf sem er einangruð úr gerjun seyði af sjaldgæfu litlu monosporum.

 

Verkunarháttur

Lífvirk styrkur carchithromycins<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.

 

Nota

Cchithromycin er öflugt frumudrepandi lyf sem getur valdið DNA tvöföldum strengjum.

 

Eituráhrif

Cachithromycin er mjög eitrað og er eitt af hundruðum umbrotsefna sem framleidd eru með jarðvegsbakteríum.

 

Lífvirkni

Calicheamicin er æxlis sýklalyf og einnig öflugt frumudrepandi lyf, sem veldur DNA tvöföldu strengjum. Calicheamicin hömlun á DNA myndun.

 

Markmið

Kalíkeamísín

 

In vitro rannsókn

Pf {{0}} (and-EFNA 4- ADC) isgeneratedViaconJugationOfHe22LysineresiduestoToAcbutdmh-n-Ac -Calicheamicin - 1 Linker-payloadWithanavergeRug-to-AntibodyRatio (Dar) of4.6.pf -06647263 Elicitsa ntigen-and-concentration-háð eituráhrifum, asexposuretopf -06647263 for96hourSresultsincelldeath (EC 50= appr1ng/ml) .cmc -544, contuspoFAhanizedCd2222222222222222222222222222222222 “ BOOKCTIVEINPEDIATRICPRIMARYB-CELLPRECURSOREDMENTMPHOBLASTICEUKIMIA (BCP-ALL) CORTHERINVITRO.CMC -544 InducescellDeathInVariousallCelllinesinadose-andtime-háð, með50ValuesRangingfr om0.15to4.9ng/ml.cmc -544 (10ng/ml) isEffectiveAndsPecificInPrimaryBcp-Allcells.incmc -544- Trea TedCells, thelevelofcd22HasDecRiEmRelativetoThatong5/44- meðhöndlaðCellSandContinedToDecRease.

 

In vivo rannsóknir

Anadccomprisingahumanizedanti-EFNA4OnoclonalantibodyConjugedTothedna-DamagingAgentCalicheamicinachievESVEREDTUMORREGCHEMICAL BookressionsInBothtnbCandovarianCancerpdXInViVo.pf -06647263 (0. 27, 0. 36mg/kg) Niðurstöður VísindasviðsantTumorRegressionsIntnbcxenografts.

 

maq per Qat: calicheamicin æxlis sýklalyf frumudrepandi lyf, Kína calicheamicin æxlis sýklalyf frumudrepandi lyf birgjar