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Selective Androgen Inhibitors Mk-1775 Oral Sarms CAS 955365-80-7

Selective Androgen Inhibitors Mk-1775 Oral Sarms CAS 955365-80-7

Basic Info Model NO.: 955365-80-7 Trademark: sendi Transport Package: Cardboard Drum Specification: 25KG/cardboard drum Origin: China HS Code: 2574120015 Product Description Product description: Description: MK-1775 information: MK-1775 inhibits Wee1 kinase in an ATP-competitive manner. Compared...

  • Features & Specification

    Basic Info

    Model NO.: 955365-80-7

    Trademark: sendi

    Transport Package: Cardboard Drum

    Specification:   25KG/cardboard drum

    Origin: China

    HS Code: 2574120015

    Product Description

    Product description:

    Product NameMK-1775
    CAS955365-80-7
    StandardEnterprise Standard
    Natural/SyntheticSynthesis
    Extraction Source0-5° Save For Research Use Only
    LevelPharmaceutical Grade
    Content99%
    Appearancewhite powder
    Packing25KG/cardboard drum
    CategoryAnimal Extracts
    IndustryPharmaceuticals
    FieldTargeted Drug Inhibitors
    Deferred ProductsCapsules, Tablets
    UseFor the treatment of certain types of ovarian cancer


     

    Description:

     

    MK-1775 information:

    MK-1775 inhibits Wee1 kinase in an ATP-competitive manner. Compared to Wee1, MK-1775 displays 2- to 3-fold less potency against Yes with IC50 of 14 nM, 10-fold less potency against seven other kinases with >80% inhibition at 1 μM, and >100-fold selectivity over human Myt 1, another kinase that inhibits cyclin-dependent kinase 1 (CDC2) by phosphorylation at an alternative site (Thr14). By abrogating the DNA damage checkpoint via blockade of Wee1 activity in WiDr cells bearing mutated p53, MK-1775 treatment inhibits the basal phosphorylation of CDC2 at Tyr15 (CDC2Y15) with EC50 of 49 nM, and suppresses gemcitabine-, carboplatin- or cisplatin-induced phosphorylation of CDC2 and cell cycle arrest in a dose-dependent manner, with EC50 of 82 nM and 81 nM, 180 nM and 163 nM, as well as 159 nM and 160 nM, respectively. MK-1775 treatment alone at 30-100 nM has no significant antiproliferative effect in WiDr and H1299 cells, whereas MK-1775 at 300 nM, sufficient to inhibit Wee1 by >80%, displays moderate but significant antiproliferative effects by 34.1% in WiDr cells and 28.4% in H1299 cells.
    in vivo: MK-1775 treatment alone at ~20 mg/kg displays minimal antitumor effects against WiDr xenografts in rats with T/C of 69% at day 3. Antitumor efficacy by MK-1775 alone in the nude rat HeLa-luc and TOV21G-shp53 xenograft models models is also moderate



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