A dual inhibitor of PI3K and BRD4
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SF2523

Item No. 21638

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-(4-morpholinyl)-7H-thieno[3,2-b]pyran-7-one
CAS Number
1174428-47-7
Molecular Formula
C19H17NO5S
Formula Weight
371.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlDMSO:PBS (pH 7.2)(1:9): 0.1 mg/mlEthanol: slightly soluble
λmax
214, 241, 306 nm
SMILES
O=C1C=C(N2CCOCC2)OC3=C1SC=C3C4=CC=C(OCCO5)C5=C4
InChi Code
InChI=1S/C19H17NO5S/c21-14-10-17(20-3-5-22-6-4-20)25-18-13(11-26-19(14)18)12-1-2-15-16(9-12)24-8-7-23-15/h1-2,9-11H,3-8H2
InChi Key
BYTKNUOMWLJVNQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $63

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    1 mg

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    5 mg

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    10 mg

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    Product Description

    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).1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Andrews, F.H., Singh, A.R., Joshi, S., et al. Dual-activity PI3K-BRD4 inhibitor for the orthogonal inhibition of MYC to block tumor growth and metastasis. Proc. Natl. Acad. Sci. USA 114(7), E1072-E1080 (2017).