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Chemical Structure| 1174428-47-7 Chemical Structure| 1174428-47-7

Structure of SF2523
CAS No.: 1174428-47-7

Chemical Structure| 1174428-47-7

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SF2523 blocks BRD4 binding to MYCN promoter PS1/PS2.

4.5 *For Research Use Only !

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Product Details of SF2523

CAS No. :1174428-47-7
Formula : C19H17NO5S
M.W : 371.41
SMILES Code : O=C1C2=C(C(C3=CC=C(OCCO4)C4=C3)=CS2)OC(N5CCOCC5)=C1
MDL No. :MFCD31382129
InChI Key :BYTKNUOMWLJVNQ-UHFFFAOYSA-N
Pubchem ID :44180156

Safety of SF2523

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of SF2523

PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • p110γ

    PI3Kγ, IC50:158 nM

  • p110α

    PI3Kα, IC50:34 nM

  • mTOR

    mTOR, IC50:280 nM

  • DNA-PK

    DNA-PK, IC50:9 nM

  • BET

    BRD4, IC50:241 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Bone marrow-derived macrophages (BMDMs) 500 nM or 1 μM 1 hour SF2523 significantly decreased the mRNA expression of IL6 and iNos in LPS induced BMDMs and gene expression of Arg, Tgfb, Vegf, Mmr, Ym1, and Fizz1 in IL4-induced BMDMs. PMC6893301
Neuroblastoma SKNBE2 cells 5 μM 24 hours To evaluate the effect of SF2523 on MYCN expression, results showed that SF2523 significantly reduced MYCN mRNA levels by approximately sevenfold. PMC5320964
Human macrophages 500 nM 24 hours SF2523 increased LC3B-II levels and decreased SQSTM1 protein levels, indicating it can overcome HIV-imposed autophagy inhibition and induce autophagy. PMC5912471
Neuroblastoma SKNBE2 cells 5 μM 30 minutes To evaluate the effect of SF2523 on the PI3K signaling pathway, results showed that SF2523 decreased MYCN and Cyclin D1 protein levels and inhibited phosphorylation of AKT at Ser473. PMC5320964
HD-MB03 cells 5.8 μM 48 hours SF2523 inhibited HD-MB03 cell proliferation with IC50 of 5.8 μM, and in combination with MDB5 significantly decreased MYCN, p-AKT, and cyclin D1 expression while increasing Bax expression PMC8573532
DAOY cells 12.6 μM 48 hours SF2523 inhibited DAOY cell proliferation with IC50 of 12.6 μM, and in combination with MDB5 significantly decreased MYCN, p-AKT, and cyclin D1 expression while increasing Bax expression PMC8573532
HD-MB03 cells 5.14 μM (IC50) 48 hours Evaluate the inhibitory effect of SF2523 on HD-MB03 cell proliferation, showing an IC50 of 5.14 μM. PMC9974792
DAOY cells 12.6 μM (IC50) 48 hours Evaluate the inhibitory effect of SF2523 on DAOY cell proliferation, showing an IC50 of 12.6 μM. PMC9974792

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NSG mice Orthotopic SHH-MB tumor model Intravenous injection 20 mg/kg Every 3 days for 3 weeks COG-133-NPs loaded with SF2523 significantly increased drug concentration in the cerebellum at 6 h (0.272 ± 0.007 ng/mg) and 24 h (0.08 ± 0.001 ng/mg), significantly inhibiting tumor growth PMC8573532
NSG mice Xenograft and orthotopic MB tumor models Intravenous injection 20 mg/kg Every third day for two weeks Evaluate the antitumor efficacy of SF2523 in MB tumor models, showing significant reduction in tumor growth and prolonged animal survival. PMC9974792
Mice (C57Bl/6, Balb/c, FVB PyMT+) Lewis lung carcinoma (LLC), CT26 colon adenocarcinoma, B16 melanoma, Panc02 pancreatic cancer, PyMT+ spontaneous breast cancer Subcutaneous injection 40 mg/kg Thrice weekly for 4 weeks SF2523 significantly suppressed tumor growth and metastasis, reduced MDSC infiltration, and increased CD8+ T cell infiltration and activity. PMC6893301
Nude mice Subcutaneous xenograft model of MYCN-amplified neuroblastoma Intraperitoneal injection 50 mg/kg Three times a week until tumors were harvested To evaluate the effect of SF2523 on tumor growth, results showed that SF2523 significantly reduced tumor volume with no gross toxicity to the mice. PMC5320964

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.69mL

0.54mL

0.27mL

13.46mL

2.69mL

1.35mL

26.92mL

5.38mL

2.69mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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