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LGK974, Porcupine (Wnt) Inhibitor

LGK974, Porcupine (Wnt) Inhibitor

$139.00
A highly potent, selective and orally bioavailable Porcupine inhibitor (Wnt signaling antagonist) in clinical trials.
Catalog No. Unit Price Qty
M60106-2s 2mg solid $139.00
M60106-2 10 mM DMSO (0.504 mL) $139.00
M60106-50s 50mg solid $950.00

Details

Product Information
Molecular Weight: 396.44
Formula: C23H20N6O
Purity: ≥98%
CAS#: 1243244-14-5
Solubility: DMSO up to 100 mM
Chemical Name: 2-(2',3-dimethyl-[2,4'-bipyridin]-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

LGK974 is a highly potent, selective and orally bioavailable Porcupine inhibitor (Wnt signaling antagonist) with an IC50 ~0.4 nM. LGK974 potently inhibits Wnt signaling in vitro and in vivo, including reduction of the Wnt-dependent LRP6 phosphorylation and the expression of Wnt target genes, such as AXIN2. LGK974 is potent and efficacious in multiple tumor models at well-tolerated doses in vivo, including murine and rat mechanistic breast cancer models driven by MMTV–Wnt1 and a human head and neck squamouscell carcinoma model (HN30). We also show that head and neck cancer cell lines with loss-of-function mutations in the Notch signaling pathway have a high response rate to LGK974. Currently LGK974 is in the Phase I study to treat cancers that are driven by the Wnt pathway in a Wnt ligand-dependent manner.

 

How to Use:

  • In vitro:  LGK974 was suggested to be used at 0.1 µM final concentration in vitro to completely block Wnt protein secretion.
  • In vivo:  LGK974 was used to dose mice orally at 0.1-10 mg/kg once or twice per day to achieve good efficacy in xenograft models.  

 

Reference:

  • 1. Liu J, et al. Targeting Wnt-driven cancer through the inhibition of Porcupine by LGK974. (2013) Proc Natl Acad Sci USA. 110(50):20224-9.
  • 2. Jiang X, et al. Inactivating mutations of RNF43 confer Wnt dependency in pancreatic ductal adenocarcinoma. (2013) Proc Natl Acad Sci USA. 110(31):12649-54. 
  • 3. Shifeng Pan. Discovery of LGK974: A selective Porcupine inhibitor targeting Wnt signaling in cancer.  AACR Annual Meeting 2013.
 
 



Products are for research use only. Not for human use.

Description

Details

Product Information
Molecular Weight: 396.44
Formula: C23H20N6O
Purity: ≥98%
CAS#: 1243244-14-5
Solubility: DMSO up to 100 mM
Chemical Name: 2-(2',3-dimethyl-[2,4'-bipyridin]-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

LGK974 is a highly potent, selective and orally bioavailable Porcupine inhibitor (Wnt signaling antagonist) with an IC50 ~0.4 nM. LGK974 potently inhibits Wnt signaling in vitro and in vivo, including reduction of the Wnt-dependent LRP6 phosphorylation and the expression of Wnt target genes, such as AXIN2. LGK974 is potent and efficacious in multiple tumor models at well-tolerated doses in vivo, including murine and rat mechanistic breast cancer models driven by MMTV–Wnt1 and a human head and neck squamouscell carcinoma model (HN30). We also show that head and neck cancer cell lines with loss-of-function mutations in the Notch signaling pathway have a high response rate to LGK974. Currently LGK974 is in the Phase I study to treat cancers that are driven by the Wnt pathway in a Wnt ligand-dependent manner.

 

How to Use:

  • In vitro:  LGK974 was suggested to be used at 0.1 µM final concentration in vitro to completely block Wnt protein secretion.
  • In vivo:  LGK974 was used to dose mice orally at 0.1-10 mg/kg once or twice per day to achieve good efficacy in xenograft models.  

 

Reference:

  • 1. Liu J, et al. Targeting Wnt-driven cancer through the inhibition of Porcupine by LGK974. (2013) Proc Natl Acad Sci USA. 110(50):20224-9.
  • 2. Jiang X, et al. Inactivating mutations of RNF43 confer Wnt dependency in pancreatic ductal adenocarcinoma. (2013) Proc Natl Acad Sci USA. 110(31):12649-54. 
  • 3. Shifeng Pan. Discovery of LGK974: A selective Porcupine inhibitor targeting Wnt signaling in cancer.  AACR Annual Meeting 2013.
 
 



Products are for research use only. Not for human use.

Reviews

  1. review Review by info@xcessbio.com
    Quality
    Price
    Value

    Question:

    I am emailing to inquire on the source of Wnt inhibitor, LGK974. We have a quote from another vendor that claims to have higher purity, so we’re trying to verify the different products’ efficacy and purity.

     

    Our support:

    LGK974 was first published in AACR 2013 Washington meeting and XcessBio synthesized it in our chemistry lab and first launched it globally in May 2012. Since then our company has been the major supplier and probably the only reliable source for this compound. The current batch of LGK974 has 99.1% purity and was tested in at least 5 labs for in vivo studies (Our customers all had positive feedbacks that the compound showed great efficacy in their animal models, especially the expensive PDX models, so they tried to purchase more. There are >50 labs bought this for in vitro studies and none complained its quality so far).  In vivo guidance and further experimental tech support will be free if purchases are made through us. 

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