1. PI3K/Akt/mTOR
    Stem Cell/Wnt
  2. GSK-3

LY2090314 (Synonyms: LY 2090314; LY-2090314)

Cat. No.: HY-16294
Handling Instructions

LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 values of 1.5 nM and 0.9 nM for GSK-3α and GSK-3β, respectively.

For research use only. We do not sell to patients.
LY2090314 Chemical Structure

LY2090314 Chemical Structure

CAS No. : 603288-22-8

Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO $135 In-stock
5 mg $120 In-stock
10 mg $190 In-stock
50 mg $550 In-stock
100 mg $950 In-stock
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500 mg   Get quote  

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Description

LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 values of 1.5 nM and 0.9 nM for GSK-3α and GSK-3β, respectively.

In Vitro

LY2090314 (20 nM) promotes a time-dependent stabilization of β-catenin total protein as well as an induction of Axin2. LY2090314 is highly selective towards GSK3 as demonstrated by its fold selectivity relative to a large panel of kinases. LY2090314 potently induces apoptotic cell death in a panel of melanoma cell lines irrespective of BRAF mutation status. Cell death induced by LY2090314 is dependent on β-catenin and GSK3β knockdown increases the sensitivity of cells to LY2090314. LY2090314 remains active in cell lines resistant to Vemurafenib and has an independent mechanism of action[2].

In Vivo

LY2090314 exhibits high clearance (approximating hepatic blood flow) and a moderate volume of distribution (appr 1-2 L/kg) resulting in rapid elimination (half-life appr 0.4, 0.7, and 1.8-3.4 hours in rats, dogs, and humans, respectively). LY2090314 is rapidly cleared by extensive metabolism with negligible circulating metabolite exposures due to biliary excretion of metabolites into feces with no apparent intestinal reabsorption[1]. LY2090314 (25 mg/kg Q3D, i.v.) elevates Axin2 gene expression in vivo, demonstrates single agent activity in the A375 xenograft model of melanoma and enhances the efficacy of DTIC[2].

Clinical Trial
Sponsor Condition Start Date Phase
Eli Lilly & Co Acute myelogenous leukemia 2010-11-30 Phase 2
Eli Lilly & Co Metastatic pancreas cancer 2013-03-31 Phase 2
Eli Lilly & Co Cancer 2007-11-30 Phase 1
References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 1.9511 mL 9.7555 mL 19.5111 mL
5 mM 0.3902 mL 1.9511 mL 3.9022 mL
10 mM 0.1951 mL 0.9756 mL 1.9511 mL
Animal Administration
[2]

LY2090314 is formulated in 20% Captisol/0.01N HCl.

Five million A375 human melanoma cancer cells are injected S.C. in the flank of female 6 to 8 week old athymic nude mice in a 1:1 mixture with matrigel. Mice are monitored daily for palpable tumors. When tumors reach appr 100 mm2 mice are randomized into groups receiving either LY2090314 (25 mg/kg Q3D) or vehicle (20% Captisol/0.01N HCl) via i.v. administration. Tumor volume (measured by calipers) and animal body weight are recorded twice weekly. Tumor volumes are calculated using the formula: (a2 × b)/2 (a being the smaller and b being the larger dimension of the tumor). For combination studies with DTIC (60 mg/kg QD), LY2090314 is dosed at 2.5 mg/kg Q3D and tumor growth monitored.

References
M.Wt

512.53

Formula

C₂₈H₂₅FN₆O₃

CAS No.

603288-22-8

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 31 mg/mL

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LY2090314
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HY-16294
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