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SF2523
CAS No. 1174428-47-7
SF2523( SF-2523 | SF 2523 )
Catalog No. M10593 CAS No. 1174428-47-7
A novel potent, dual inhibitor of PI3K and BRD4 with IC50 of 241, 34, 158 nM for BRD4 (BD1), PI3Kα and PI3Kγ, respectively.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 75 | In Stock |
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| 5MG | 68 | In Stock |
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| 10MG | 116 | In Stock |
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| 25MG | 275 | In Stock |
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| 50MG | 423 | In Stock |
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| 100MG | 625 | In Stock |
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| 200MG | Get Quote | In Stock |
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| 500MG | 1330 | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NameSF2523
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NoteResearch use only, not for human use.
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Brief DescriptionA novel potent, dual inhibitor of PI3K and BRD4 with IC50 of 241, 34, 158 nM for BRD4 (BD1), PI3Kα and PI3Kγ, respectively.
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DescriptionA novel potent, dual inhibitor of PI3K and BRD4 with IC50 of 241, 34, 158 nM for BRD4 (BD1), PI3Kα and PI3Kγ, respectively; interacts robustly with the full-length BRD4 (Kd=140 nM) and BRD4(BD1) (Kd=150 nM), binds more weakly BRD4(BD2) (Kd = 710 nM); blocks MYC expression and activation, promotes MYC degradation, and markedly inhibits cancer cell growth and metastasis both in vitro and in vivo.
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In VitroSF2523 treatment decreases protein levels of MYCN and Cyclin D1, the MYCN target, and inhibits AKT activation by blocking phosphorylation of AKT at Ser473. SF2523 treatment leads to the displacement of BRD4 from both MYCN promoter sites. SF2523 interacts robustly with the full-length BRD4 (Kd=140 nM) and exhibits comparable affinity to the BRD4 first BD (BD1) (Kd=150 nM), however it binds more weakly to the second BD (BD2) of BRD4 (Kd=710 nM). Comparison of binding affinities of SF2523 for BDs of other proteins reveal that it binds equally well to BDs of BRD4, BRD2, and BRD3; shows moderate binding to BDs of CECR2 and BRDT; but associates much weaker with other BDs.
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In VivoSF2523 treatment results in a significant reduction of tumor volume compared with control. Importantly, SF2523 shows no gross toxicity to the treated mice, as there is no notable change in body weight. Tumors from SF2523-treated mice have markedly reduced MYCN, pAKT, and Cyclin D1 levels compared with levels of these proteins in vehicle-treated mice tumors.
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SynonymsSF-2523 | SF 2523
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PathwayPI3K/Akt/mTOR signaling
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TargetPI3K
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RecptorBRD4|DNA-PK|mTOR|PI3Kα|PI3Kγ
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Research Area——
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Indication——
Chemical Information
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CAS Number1174428-47-7
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Formula Weight371.40698
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Molecular FormulaC19H17NO5S
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Purity>98% (HPLC)
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SolubilityDMSO: ≥ 30 mg/mL
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SMILESO=C1C=C(N2CCOCC2)OC3=C1SC=C3C4=CC=C(OCCO5)C5=C4
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Chemical Name7H-Thieno[3,2-b]pyran-7-one, 3-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-(4-morpholinyl)-
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Andrews FH, et al. Proc Natl Acad Sci U S A. 2017 Feb 14;114(7):E1072-E1080.
2. Carlino L, et al. J Med Chem. 2016 Oct 27;59(20):9305-9320.
3. Shen G, et al. Biochem Biophys Res Commun. 2017 Nov 10. pii: S0006-291X(17)32240-4.
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