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SH-4-54

Cat. No. M3664
SH-4-54 Structure
Size Price Availability Quantity
2mg USD 105 In stock
5mg USD 160 In stock
10mg USD 250 In stock
25mg USD 485 In stock
50mg USD 720 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

SH-4-54 strongly binds to STAT3 protein (K D = 300 nM). SH-4-54 potently kills glioblastoma brain cancer stem cells (BTSCs) and effectively suppresses STAT3 phosphorylation and its downstream transcriptional targets at low nM concentrations. SH-4-54 exhibites blood-brain barrier permeability, potently controlled glioma tumor growth, and inhibites pSTAT3 in vivo.

Protocol
Cell Experiment
Cell lines BTSC lines 25M, 67EF, 73EF, 84EF and 127EF
Preparation method Dissociating BTSC spheres to single cells with the enzyme Accumax, seeding at 1500 cells/ 96-well and treating with drug or vehicle (DMSO) one day after plating. Repeating cytotoxicity studies independently using BTSC lines 25M, 67EF, 73EF, 84EF and 127EF.Dissociating BTSC spheres to single cells as above and plating in 96 well plates in triplicate at 3000 cells/ 96-well. In both sets of experiments using drugs as serial dilutions within the range of 5 μM to 100 nM in the first set and 25 μM to 10 nM. Assessing cell viability following drug treatment three days later using the alamarBlue assay according to the manufacturer’s instructions. All culture experiments are performed in triplicate with a minimum of three wells per condition
Concentrations ~25 μM
Incubation time 72 hours
Animal Experiment
Animal models NOD-SCID bearing ed with BT73 glioma xenografts
Formulation 10 mg/kg
Dosages Suspended in 50% polyethylene glycol 300 in water
Administration i.p.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 610.59
Formula C29H27F5N2O5S
CAS Number 1456632-40-8
Purity >99%
Solubility DMSO
Storage at -20°C
References

Potent Targeting of the STAT3 Protein in Brain Cancer Stem Cells: A Promising Route for Treating Glioblastoma.
Haftchenary S, et al. ACS Med Chem Lett. 2013 Sep 8;4(11):1102-7. PMID: 24900612.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SH-4-54 supplier, STAT, inhibitors

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