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10058-F4

Cat. No. M2352
10058-F4 Structure
Size Price Availability Quantity
10mg USD 80 In stock
25mg USD 120 In stock
50mg USD 220 In stock
100mg USD 380 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

10058-F4 inhibits the growth of leukemic cells and dimerization of the c-Myc/Max heterodimerization to control the cell proliferation, apoptosis, and differentiation, and its aberrant expression. 10058-F4 increased FOXO1 mRNA in MedB-1 cells. 10058-F4 is most efficient in inducing neuronal differentiation and lipid accumulation in MYCN-amplified neuroblastoma cells. 10058-F4 could markedly suppresse the wild-type LKB1 loss-induced cell invasiveness. 10058-F4 increased the chemosensitivity of HepG2 cells to low-dose doxorubicin, 5-fluorouracil and cisplatin.

Protocol
Cell Experiment
Cell lines PC-3 and DU145 cells
Preparation method MTT assay
PC-3 cells (2 × 104 cells in logarithmic growth) were plated into 96-well culture plates and allowed to adhere to the plates for 24 h prior to the addition of 10058-F4 in medium containing 1% ethanol such that the final concentrations in the wells were 0.1-100 μM in medium containing 0.3% ethanol. After 72 h, 50 μl of 1 mg/ml MTT was added to each well. The cells were washed with medium and phosphate buffered saline, and 150 μl of DMSO was added to each well, followed by shaking for 5 min. The absorbance at 570 nm was read on DYNEX MRX Revelation microplate reader (Dynex, Vienna, VA, USA). Results were compared to wells containing cells treated with vehicle alone and were expressed as % inhibition. The IC50 was calculated using the Hill equation, the program ADAPT II, and data from three separate experiments.
Concentrations 0.1-100 μM
Incubation time 72 h
Animal Experiment
Animal models SCID mice bearing DU145 or PC-3 xenografts
Formulation cremophor EL:ethanol:saline (1:1:8 v/v/v) at a final concentration of 2 or 3 mg/ml
Dosages 20 or 30 mg/kg daily for 5 days for 2 weeks
Administration i.v.
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 249.35
Formula C12H11NOS2
CAS Number 403811-55-2
Purity >99%
Solubility DMSO 40 mg/mL
Storage at -20°C
References

Targeting of the MYCN Protein with Small Molecule c-MYC Inhibitors.
Müller I, et al. PloS one. 2014 May 23;9(5):e97285. PMID: 24859015.

The MZF1/c-MYC axis mediates lung adenocarcinoma progression caused by wild-type lkb1 loss.
Tsai LH, et al. Oncogene. 2014 May 5. PMID: 24793789.

Efficacy, pharmacokinetics, tisssue distribution, and metabolism of the Myc-Max disruptor, 10058-F4 [Z,E]-5-[4-ethylbenzylidine]-2-thioxothiazolidin-4-one, in mice.
Guo J, et al. Cancer Chemother Pharmacol. 2009 Mar;63(4):615-25. PMID: 18509642.

Small-molecule c-Myc inhibitor, 10058-F4, inhibits proliferation, downregulates human telomerase reverse transcriptase and enhances chemosensitivity in human hepatocellular carcinoma cells.
Lin CP, et al. Anticancer Drugs. 2007 Feb;18(2):161-170. PMID: 17159602.

A small-molecule c-Myc inhibitor, 10058-F4, induces cell-cycle arrest, apoptosis, and myeloid differentiation of human acute myeloid leukemia.
Huang MJ, et al. Experimental hematology. 2006 Nov;34(11):1480-9. PMID: 17046567.

Related c-Myc Products
10074-G5

10074-G5 is a c-Myc/Max interaction inhibitor, which binds to a different specific binding site (region) of C-Myc than 10054-F4.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: 10058-F4 supplier, c-Myc, inhibitors

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