A dual inhibitor of PI3K and BRD4 (IC50s = 16

SF2523 – 1 mg

Brand:
Cayman
CAS:
1174428-47-7
Storage:
-20
UN-No:
Non-Hazardous - /

SF2523 is a dual inhibitor of phosphatidylinositol 3-kinase (PI3K; IC50 = 16 nM) and bromodomain-containing protein 4 (BRD4; IC50s = 241 and 1,550 nM for BRD4 bromodomains 1 and 2, respectively).{33478} It reduces MYCN gene expression, decreases MYCN and cyclin D1 protein levels, and inhibits phosphorylation of Akt in SKNBE2 cells. In vivo, SF2523 reduces tumor volume and protein levels of MYCN and cyclin D1 in a MYCN-amplified SKNBE2 neuroblastoma xenograft model in mice. It also reduces tumor growth and the number of colonic lymph node metastases in the murine orthotopic pancreatic Panc02 carcinoma model for spontaneous lymph node metastasis.  

 

Out of stock

Add to quotes
SKU: 21638 - Category:

Description

A dual inhibitor of PI3K and BRD4 (IC50s = 16, and 241 and 1,550 nM for PI3K, and BRD4 bromodomains 1 and 2, respectively); reduces MYCN gene expression and decreases MYCN and cyclin D1 protein levels; inhibits phosphorylation of Akt in SKNBE2 cells; reduces tumor volume and protein levels of MYCN and cyclin D1 in a MYCN-amplified SKNBE2 neuroblastoma xenograft model in mice; reduces tumor growth and the number of colonic lymph node metastases in the murine orthotopic pancreatic Panc02 carcinoma model

Formal name: 3-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-(4-morpholinyl)-7H-thieno[3,2-b]pyran-7-one

Synonyms: 

Molecular weight: 371.4

CAS: 1174428-47-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|PI3K||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling

Related products

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

    (R)-Roscovitine – 1 mg

    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 - 1 mg

    Available on backorder

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

    1,2-Dipalmitoyl-sn-glycero-3-PC – 250 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 - 250 mg

    Available on backorder

    Add to quotes
    View product page
  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 250 mg

    The tetracycline repressor (TetR) is a transcriptional regulator which normally binds tightly to its palindromic tetO operator DNA, blocking gene expression.{17508} Tet causes the repressor to dissociate from the DNA, allowing transcription to occur. A novel reverse TetR (revTetR) requires tetracycline as a co-repressor to bind tetO and block transcription.{17509,17510} Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet.{17508,17511} Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet,{17512} so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.{17508}  

     

    Brand:
    Cayman
    SKU:10009542 - 250 mg

    Available on backorder

    Add to quotes
    View product page
  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 50 mg

    The tetracycline repressor (TetR) is a transcriptional regulator which normally binds tightly to its palindromic tetO operator DNA, blocking gene expression.{17508} Tet causes the repressor to dissociate from the DNA, allowing transcription to occur. A novel reverse TetR (revTetR) requires tetracycline as a co-repressor to bind tetO and block transcription.{17509,17510} Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet.{17508,17511} Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet,{17512} so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.{17508}  

     

    Brand:
    Cayman
    SKU:10009542 - 50 mg

    Available on backorder

    Add to quotes
    View product page