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Signaling Pathway

LY2090314

HY-16294

(LY 2090314; LY-2090314)

LY2090314

LY2090314 Chemical Structure

LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50s of 1.5 nM and 0.9 nM for GSK-3α and GSK-3β respectively.

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
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO €132 In-stock
5 mg €118 In-stock
10 mg €186 In-stock
50 mg €539 In-stock
100 mg €931 In-stock
200 mg Get quote
500 mg Get quote

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Inquiry Information
Product name: LY2090314
Cat. No.: HY-16294

LY2090314 Data Sheet

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    Purity: 99.73%

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Biological Activity of LY2090314

LY2090314  is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50s of 1.5 nM and 0.9 nM for GSK-3α and GSK-3β respectively.
IC50 Value: 1.5 nM (GSK-3α); 0.9 nM (GSK-3β) [1]
Target: GSK-3α; GSK-3β
LY2090314  is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) which plays an important role in many pathways, including initiation of protein synthesis, cell proliferation, cell differentiation, and apoptosis.
in vitro: LY2090314 selectively inhibits the activity of GSK-3 by interrupting ATP binding. LY2090314 is able to stabilize β-catenin. LY2090314 shows limited efficacy as monotherapy. LY3090314 enhances the efficacy of cisplatin and carboplatin in solid tumor cancer cell lines in vitro.
in vivo: Even in Mdr1a-, Bcrp-, and Mrp2-knockout rats, LY2090314 metabolites did not appear in circulation, and their urinary excretion was not enhanced, because the hypothesized impaired biliary excretion of metabolites in the absence of these canalicular transporters was not observed. Canine metabolite disposition was generally similar, with the notable exception of dog-unique LY2090314 glucuronide [1].
Toxicity:
Clinical trial: A Study of LY-2090314 and Chemotherapy in Participants With Metastatic Pancreatic Cancer. Phase1/2
 

Chemical Information

M.Wt 512.53 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C28H25FN6O3
CAS No 603288-22-8
Solvent & Solubility

DMSO: ≥ 31 mg/mL

Preparing Stock Solutions

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

Clinical Information of LY2090314

Product Name Sponsor Only Condition Start Date End Date Phase Last Change Date
LY2090314 Eli Lilly & Co Acute myelogenous leukemia 30-NOV-10 31-DEC-12 Phase 2 13-MAY-13
Eli Lilly & Co Metastatic pancreas cancer 31-MAR-13 31-MAY-17 Phase 2 01-OCT-13
Eli Lilly & Co Cancer 30-NOV-07 30-APR-11 Phase 1 02-AUG-11

References on LY2090314

Inhibitor Kit

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