[CAS NO. 1174428-47-7] SF2523

Name: SF2523
Brand: Arctom Scientific
SKU: SLK-S8589

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PRODUCTS SPECIFICATIONS [1174428-47-7]

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Catalog

SLK-S8589

Brand

Selleck

CAS

1174428-47-7

DESCRIPTION [1174428-47-7]

Overview

MDL	MFCD31382129
Molecular Weight	371.41
Molecular Formula	C19H17NO5S
SMILES	O=C1C2=C(C(C3=CC=C(OCCO4)C4=C3)=CS2)OC(N5CCOCC5)=C1

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.6924 mL	13.4622 mL	26.9244 mL
5 mM	0.5385 mL	2.6924 mL	5.3849 mL
10 mM	0.2692 mL	1.3462 mL	2.6924 mL
50 mM	0.0538 mL	0.2692 mL	0.5385 mL

Description

SF2523 is a highly selective and potent inhibitor of with IC50 values of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for , respectively.

Targets

DNA-PK ^[1] (Cell-free assay)	PI3Kα ^[1] (Cell-free assay)	PI3Kγ ^[1] (Cell-free assay)	BRD4 ^[1] (Cell-free assay)	mTOR ^[1] (Cell-free assay)
9 nM	34 nM	158 nM	241 nM	280 nM

In vitro

SF2523 blocks BRD4 binding to MYCN promoter PS1/PS2. It blocks M1-M2 transition and decreases levels of p-AKT, N-MYC in several neuroblastoma cell lines. SF2523 treatment decreases protein levels of MYCN and Cyclin D1, the MYCN target, and inhibits AKT activation by blocking phosphorylation of AKT at Ser473. 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 reveals 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.

In vivo

SF2523 blocks spontaneous metastasis and tumor growth. SF2523 has demonstrated animal efficacy results without toxicity in the following 4 animal models: orthotopic pancreatic model, multiple myeloma model, renal cell carcinoma model, neuroblastoma xenograft model. SF2523 targets PI3K-driven and BRD4-driven oncogenic pathways in vivo. SF2523 is less toxic to the host organism in vivo than a combination of an equipotent PI3K inhibitor and BRD4 inhibitor.

References

[1] Luca Carlino, et al. J Med Chem. 2016, 59 (20): pp 9305–9320.
[2] Alok Singh, et al. AACR Cancer Res. 2016, 76(14 Suppl):Abstract nr LB-211.
[3] Andrews FH, et al. Proc Natl Acad Sci U S A. 2017, 114(7):E1072-E1080.