A dual inhibitor of PI3K and BRD4 (IC50s = 16

SF2523 – 10 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.  

 

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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

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