A dual inhibitor of PI3K and mTOR (IC50s = 3.4

GNE-493 – 10 mg

Brand:
Cayman
CAS:
1033735-94-2
Storage:
-20
UN-No:
Non-Hazardous - /

GNE-493 is a dual inhibitor of PI3K and mammalian target of rapamycin (mTOR; IC50s = 3.4, 12, 16, 16, and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, and mTOR, respectively).{24603} It inhibits proliferation of PC3 and MCF-7.1 cells with IC50 values of 330 and 180 nM, respectively. GNE-493 (10 mg/kg per day) reduces tumor volume in PC3 and MCF-7.1 mouse xenograft models, which are PTEN negative or PI3Kα activating mutation positive, respectively. It also decreases relative levels of phosphorylated Akt, PRAS40, and S6RP in tumor tissue in the MCF-7.1 mouse xenograft model.  

 

Available on backorder

Add to quotes
SKU: 29224 - 10 mg Category:

Description

A dual inhibitor of PI3K and mTOR (IC50s = 3.4, 12, 16, and 16 nM for PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively); inhibits proliferation of PC3 and MCF-7.1 cells (IC50s = 330 and 180 nM, respectively); reduces tumor volume in PC3 and MCF-7.1 mouse xenograft models at 10 mg/kg per day

Formal name: 2-(2-amino-5-pyrimidinyl)-α,α-dimethyl-4-(4-morpholinyl)-thieno[3,2-d]pyrimidine-6-methanol

Synonyms: 

Molecular weight: 372.4

CAS: 1033735-94-2

Purity: ≥98%

Formulation: A crystalline solid

Related products

  • A potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM; also inhibits Cdk7/cyclin H

    (R)-Roscovitine – 500 µg

    Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}  

     

    Brand:
    Cayman
    SKU:10009569 - 500 µg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 100 mg

    1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}  

     

    Brand:
    Cayman
    SKU:10009473 - 100 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 50 mg

    1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}  

     

    Brand:
    Cayman
    SKU:10009473 - 50 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}

    CAY10512 – 50 mg

    The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}  

     

    Brand:
    Cayman
    SKU:10009536 - 50 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page