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LY2090314

Cat. No. M2826
LY2090314 Structure
Size Price Availability Quantity
5mg USD 105  USD105 In stock
10mg USD 165  USD165 In stock
50mg USD 480  USD480 In stock
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Quality Control & Documentation
Biological Activity

LY2090314 is a potent GSK-3 inhibitor for GSK-3α/β with IC50 of 1.5 nM/0.9 nM; may improve the efficacy of platinum-based chemotherapy regimens. Phase 1/2.

Customer Product Validations & Biological Datas
Source BMC Cancer (2018). Figure 2. LY2090314
Method MTT assay
Cell Lines SH-SY-5Y cells
Concentrations 10, 20, and 50 nM
Incubation Time 48, 72, and 96 h
Results In Fig. 1a, a steep reduction on average of 23% at 48 h, 42% at 72 h, and 61% at 96 h was noted in NGP cells treated with 20 nM of LY2090314.
Chemical Information
Molecular Weight 512.53
Formula C28H25FN6O3
CAS Number 603288-22-8
Solubility (25°C) DMSO 10 mM
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] Alessio Reggio, et al. Adipogenesis of skeletal muscle fibro/adipogenic progenitors is affected by the WNT5a/GSK3/β-catenin axis

[2] Guoxu Fang, et al. Inhibition of GSK-3β activity suppresses HCC malignant phenotype by inhibiting glycolysis via activating AMPK/mTOR signaling

[3] Selvi Kunnimalaiyaan, et al. Antiproliferative and apoptotic effect of LY2090314, a GSK-3 inhibitor, in neuroblastoma in vitro

[4] Jennifer M Atkinson, et al. Activating the Wnt/β-Catenin Pathway for the Treatment of Melanoma--Application of LY2090314, a Novel Selective Inhibitor of Glycogen Synthase Kinase-3

[5] Maciej J Zamek-Gliszczynski, et al. Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure

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  Catalog
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Keywords: LY2090314 supplier, GSK-3, inhibitors, activators


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