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WAY-600

Cat. No. M1852
WAY-600 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 110  USD110 In stock
5mg USD 200  USD200 In stock
10mg USD 280  USD280 In stock
50mg USD 740  USD740 In stock
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Quality Control & Documentation
Biological Activity

WAY-600 is a selective single digit nanomolar ATP-competitive mTOR inhibitor with an IC50 of about 9 nM. It has significant selectivity for these enzymes over phosphatidylinositol 3-kinase (PI3K) isofoms (>100-fold). With the 11% suppression by rapamycin, WAY-600 treated HEK293 cells indicated a 50% inhibition of polysomes. And WAY-600 blocked mTORC2-dependent phosphorylation of AKT in vitro and in vivo acutely. Without significant inhibition of P-AKT(T308), WAY-600 inhibited the mTORC1 substrate P-S6K(T389) and mTORC2 substrate P-AKT(S473) at submicromolar concentrations in various cancer cells.

Customer Product Validations & Biological Datas
Source Biochem Biophys Res Commun (2016). Figure 1.WAY-600
Method MTT viability
Cell Lines HCC cell
Concentrations 10`1000 nM
Incubation Time 48 h
Results Results in Fig. 1A showed thatWAY-600, at 10e1000 nM, significantly decreased MTT viability OD of HepG2 cells.
Protocol (for reference only)
Cell Experiment
Cell lines MDA361 and U87MG cells
Preparation method Cell lines of Rat1, HEK293, MDA-MB-361, MDA-MB-468, MDA-MB-231, LNCap, DU145, U87MG, A498, HCT116, and HT29 were obtained from the American Type Culture Collection. PC3MM2 was obtained from Dr. Carolyn Discafani (Wyeth Discovery Oncology). All cells were cultured using standard cell culture methods. For tumor cell growth assays, cells were plated in 96-well culture plates at 1000 to 3000 cells per well for 24 h, treated with DMSO or various doses of mTOR inhibitors. Viable cell densities were determined three days later by MTS assay employing an assay kit (CellTiter 96® AQueous, Cat # G5421, Promega) following the kit assay protocol. The effect of each treatment was calculated as percent of control growth relative to the DMSO-treated cells grown in the same culture plate. Inhibitor dose response curves were plotted for determination of IC50 values.
Concentrations 0.01~100 μM
Incubation time 3 days
Animal Experiment
Animal models PC3MM2 tumors xenograft model in BALB/c nu/nu female mice
Formulation 5% ethanol, 5% polysorbate 80, 5% polyethylene glycol-400
Dosages 50mg/kg on days 0 to 4 once daily or twice daily
Administration i.p.
Chemical Information
Molecular Weight 494.59
Formula C28H30N8O
CAS Number 1062159-35-6
Solubility (25°C) DMSO ≥ 21 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Yu K, et al. Cancer Res. Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin.

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Keywords: WAY-600 supplier, mTOR, inhibitors, activators


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