Determine the necessary mass, volume, or concentration for preparing a solution.
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
≥97% for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Store at -20°C Ships Ice chest + Ice pads Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Information
SF2523 is a highly selective and potent inhibitor ofPI3Kwith IC50 values of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM forPI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
Targets
DNA-PK (Cell-free assay); PI3Kα (Cell-free assay); PI3Kγ (Cell-free assay); BRD4 (Cell-free assay); mTOR (Cell-free assay)
;9 nM; 34 nM; 158 nM; 241 nM; 280 nMIn 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.
Cell Research(from reference)
Cell lines:neuroblastoma SKNBE2 cell line
Concentrations:5 μM
Incubation Time:24 h
| ALogP | 3.081 |
|---|---|
| Legame rotabile | 2 |
| Pubchem Sid | 504770295 |
|---|---|
| Pubchem Sid Url | https://pubchem.ncbi.nlm.nih.gov/substance/504770295 |
| Sorrisi canonici | C1COCCN1C2=CC(=O)C3=C(O2)C(=CS3)C4=CC5=C(C=C4)OCCO5 |
| IUPAC Name | 3-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-morpholin-4-ylthieno[3,2-b]pyran-7-one |
| InChIKey | BYTKNUOMWLJVNQ-UHFFFAOYSA-N |
| 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 |
| Isomeri SMILES | C1COCCN1C2=CC(=O)C3=C(O2)C(=CS3)C4=CC5=C(C=C4)OCCO5 |
| PubChem CID | 44180156 |
| Peso molecolare | 371.41 |
Comprehensive hazard, handling, storage, and regulatory compliance document.
Download SDS →Lot-specific quality data. Enter your lot number to retrieve the exact COA.
Look up COA →Full quality attributes and acceptance criteria for this grade.
View spec sheet →Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organoheterocyclic compounds |
| Classe | Benzodioxanes |
| Subclass | Benzo-1,4-dioxanes |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Benzo-1,4-dioxanes |
| Alternative Parents | Dialkylarylamines Pyranones and derivatives Alkyl aryl ethers Para dioxins Morpholines Benzenoids Vinylogous amides Thiophenes Heteroaromatic compounds Oxacyclic compounds Dialkyl ethers Azacyclic compounds Organic oxides Hydrocarbon derivatives |
| Molecular Framework | Aromatic heteropolycyclic compounds |
| Substituents | Benzo-1,4-dioxane - Dialkylarylamine - Alkyl aryl ether - Pyranone - Morpholine - Oxazinane - Para-dioxin - Pyran - Benzenoid - Thiophene - Vinylogous amide - Heteroaromatic compound - Tertiary amine - Dialkyl ether - Ether - Azacycle - Oxacycle - Organic oxygen compound - Organic oxide - Amine - Organooxygen compound - Organonitrogen compound - Organic nitrogen compound - Hydrocarbon derivative - Aromatic heteropolycyclic compound |
| Descrizione | This compound belongs to the class of organic compounds known as benzo-1,4-dioxanes. These are heterocyclic compounds containing a benzene ring fused to a 1,4-dioxane ring. |
| External Descriptors | Not available |
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
| Solubilità | Solubility (25°C) In vitro DMSO: 29 mg/mL (78.08 mM); Ethanol: 7 mg/mL (18.84 mM); Water: Insoluble; |
|---|---|
| DMSO (mg/mL) Solubilità massima | 29 |
| DMSO (mM) Solubilità massima | 78.08082712 |
| Acqua (mg/mL) Solubilità massima | <1 |
| Peso molecolare | 371.400 g/mol |
| XLogP3 | 2.900 |
| Hydrogen Bond Donor Count | 0 |
| Hydrogen Bond Acceptor Count | 7 |
| Rotatable Bond Count | 2 |
| Exact Mass | 371.083 Da |
| Monoisotopic Mass | 371.083 Da |
| Topological Polar Surface Area | 85.500 Ų |
| Heavy Atom Count | 26 |
| Formal Charge | 0 |
| Complexity | 578.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 1 |