SF2523
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MedKoo CAT#: 206841

CAS#: 1174428-47-7

Description: SF2523 is a highly selective and potent dual pan-PI3K/BRD4 inhibitor. SF2523 exhibits a remarkable kinase selectivity inhibiting potently only 4 out of the 232 non-PI3K kinases at the enzyme level, showing broad potency against 19 cancer cell lines in vitro, and exhibiting potent in vivo anti- tumor activity in xenograft studies. SF2523 exhibits demonstrated anti- cancer stem cell and generation of oxidative stress activities. The biological, chemical, and computational profile of SF2523 have been published in J. Med. Chem. 2013, Vol. 56, pages 1922-1939 (doi: 10.1021/jm301522m).


Chemical Structure

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SF2523
CAS# 1174428-47-7

Theoretical Analysis

MedKoo Cat#: 206841
Name: SF2523
CAS#: 1174428-47-7
Chemical Formula: C19H17NO5S
Exact Mass: 371.08
Molecular Weight: 371.407
Elemental Analysis: C, 61.44; H, 4.61; N, 3.77; O, 21.54; S, 8.63

Price and Availability

Size Price Availability Quantity
5mg USD 90 Ready to ship
10mg USD 150 Ready to ship
25mg USD 345 Ready to ship
50mg USD 600 Ready to ship
100mg USD 1050 Ready to ship
200mg USD 1850 Ready to ship
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Synonym: SF2523; SF-2523; SF 2523.

IUPAC/Chemical Name: 3-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-5-morpholino-7H-thieno[3,2-b]pyran-7-one

InChi Key: BYTKNUOMWLJVNQ-UHFFFAOYSA-N

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

SMILES Code: O=C1C=C(N2CCOCC2)OC3=C1SC=C3C4=CC=C(OCCO5)C5=C4

Appearance: Red solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target: SF2523 is an inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
In vitro activity: Targeting PI3K-Akt-mTOR and BRD4 by SF2523 potently inhibited chondrosarcoma cell growth. SF2523 potently inhibited survival, proliferation and migration, and induced apoptosis activation in SW1353 cells and primary human chondrosarcoma cells. SF2523 was non-cytotoxic to the primary human osteoblasts and OB-6 osteoblastic cells. SF2523 blocked Akt-mTOR activation and downregulated BRD4-regulated genes in chondrosarcoma cells. Reference: Biochem Biophys Res Commun. 2019 Apr 9;511(3):559-565. https://pubmed.ncbi.nlm.nih.gov/30824188/
In vivo activity: SF2523 decreased tumor growth and immunosuppressive macrophage polarization in the orthotopic Panc02 mouse model. Net tumor weight and immunosuppressive macrophage polarization was strongly reduced in mammary tumors from the SF2523-treated mice. Tumor progression was also inhibited in SF2523-treated PYMT tumor model animals. Reference: Mol Cancer Ther. 2019 Jun;18(6):1036-1044. https://pubmed.ncbi.nlm.nih.gov/31018997/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMF 10.0 26.92
DMSO 29.5 79.43
DMSO:PBS (pH 7.2) (1:9) 0.1 0.27
Ethanol 7.0 18.85

Preparing Stock Solutions

The following data is based on the product molecular weight 371.41 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Zhu JX, Xiao JR. SF2523 inhibits human chondrosarcoma cell growth in vitro and in vivo. Biochem Biophys Res Commun. 2019 Apr 9;511(3):559-565. doi: 10.1016/j.bbrc.2019.02.080. Epub 2019 Feb 26. PMID: 30824188. 2. Goldin AN, Singh A, Joshi S, Jamieson C, Durden DL. Augmented Antitumor Activity for Novel Dual PI3K/BDR4 Inhibitors, SF2523 and SF1126 in Ewing Sarcoma. J Pediatr Hematol Oncol. 2021 Apr 1;43(3):e304-e311. doi: 10.1097/MPH.0000000000002054. PMID: 33480647. 3. Joshi S, Singh AR, Liu KX, Pham TV, Zulcic M, Skola D, Chun HB, Glass CK, Morales GA, Garlich JR, Durden DL. SF2523: Dual PI3K/BRD4 Inhibitor Blocks Tumor Immunosuppression and Promotes Adaptive Immune Responses in Cancer. Mol Cancer Ther. 2019 Jun;18(6):1036-1044. doi: 10.1158/1535-7163.MCT-18-1206. Epub 2019 Apr 24. PMID: 31018997; PMCID: PMC6893301. 4. Shen G, Jiang M, Pu J. Dual inhibition of BRD4 and PI3K by SF2523 suppresses human prostate cancer cell growth in vitro and in vivo. Biochem Biophys Res Commun. 2018 Jan 1;495(1):567-573. doi: 10.1016/j.bbrc.2017.11.062. Epub 2017 Nov 10. PMID: 29133261.
In vitro protocol: 1. Zhu JX, Xiao JR. SF2523 inhibits human chondrosarcoma cell growth in vitro and in vivo. Biochem Biophys Res Commun. 2019 Apr 9;511(3):559-565. doi: 10.1016/j.bbrc.2019.02.080. Epub 2019 Feb 26. PMID: 30824188. 2. Goldin AN, Singh A, Joshi S, Jamieson C, Durden DL. Augmented Antitumor Activity for Novel Dual PI3K/BDR4 Inhibitors, SF2523 and SF1126 in Ewing Sarcoma. J Pediatr Hematol Oncol. 2021 Apr 1;43(3):e304-e311. doi: 10.1097/MPH.0000000000002054. PMID: 33480647.
In vivo protocol: 1. Joshi S, Singh AR, Liu KX, Pham TV, Zulcic M, Skola D, Chun HB, Glass CK, Morales GA, Garlich JR, Durden DL. SF2523: Dual PI3K/BRD4 Inhibitor Blocks Tumor Immunosuppression and Promotes Adaptive Immune Responses in Cancer. Mol Cancer Ther. 2019 Jun;18(6):1036-1044. doi: 10.1158/1535-7163.MCT-18-1206. Epub 2019 Apr 24. PMID: 31018997; PMCID: PMC6893301. 2. Shen G, Jiang M, Pu J. Dual inhibition of BRD4 and PI3K by SF2523 suppresses human prostate cancer cell growth in vitro and in vivo. Biochem Biophys Res Commun. 2018 Jan 1;495(1):567-573. doi: 10.1016/j.bbrc.2017.11.062. Epub 2017 Nov 10. PMID: 29133261.

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1: Joshi S, Singh AR, Liu KX, Pham TV, Zulcic M, Skola D, Chun HB, Glass CK, Morales GA, Garlich JR, Durden DL. SF2523: Dual PI3K/BRD4 Inhibitor Blocks Tumor Immunosuppression and Promotes Adaptive Immune Responses in Cancer. Mol Cancer Ther. 2019 Jun;18(6):1036-1044. doi: 10.1158/1535-7163.MCT-18-1206. Epub 2019 Apr 24. PubMed PMID: 31018997.

2: Zhu JX, Xiao JR. SF2523 inhibits human chondrosarcoma cell growth in vitro and in vivo. Biochem Biophys Res Commun. 2019 Apr 9;511(3):559-565. doi: 10.1016/j.bbrc.2019.02.080. Epub 2019 Feb 26. PubMed PMID: 30824188.

3: Campbell GR, Bruckman RS, Herns SD, Joshi S, Durden DL, Spector SA. Induction of autophagy by PI3K/MTOR and PI3K/MTOR/BRD4 inhibitors suppresses HIV-1 replication. J Biol Chem. 2018 Apr 20;293(16):5808-5820. doi: 10.1074/jbc.RA118.002353. Epub 2018 Feb 23. PubMed PMID: 29475942; PubMed Central PMCID: PMC5912471.

4: Zhu H, Mao JH, Wang Y, Gu DH, Pan XD, Shan Y, Zheng B. Dual inhibition of BRD4 and PI3K-AKT by SF2523 suppresses human renal cell carcinoma cell growth. Oncotarget. 2017 Sep 30;8(58):98471-98481. doi: 10.18632/oncotarget.21432. eCollection 2017 Nov 17. PubMed PMID: 29228703; PubMed Central PMCID: PMC5716743.

5: Su J, Liu X, Zhang S, Yan F, Zhang Q, Chen J. A theoretical insight into selectivity of inhibitors toward two domains of bromodomain-containing protein 4 using molecular dynamics simulations. Chem Biol Drug Des. 2018 Mar;91(3):828-840. doi: 10.1111/cbdd.13148. Epub 2017 Dec 10. PubMed PMID: 29139214.

6: Shen G, Jiang M, Pu J. Dual inhibition of BRD4 and PI3K by SF2523 suppresses human prostate cancer cell growth in vitro and in vivo. Biochem Biophys Res Commun. 2018 Jan 1;495(1):567-573. doi: 10.1016/j.bbrc.2017.11.062. Epub 2017 Nov 10. PubMed PMID: 29133261.