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WNT-974

CAT: 0013-GTR19164189-07Size: 25 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19164189-07Size:25 mg
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Description
A potent and specific small-molecule Porcupine (PORCN) inhibitor with IC50 of 1 nM in the PORCN radioligand binding assay; potently inhibits Wnt signaling with IC50 of 0.4 nM, with no major cytotoxicity; reduces Wnt-dependent LRP6 phosphorylation and the expression of Wnt target genes, such as AXIN2; is potent and efficacious in multiple tumor models at well-tolerated doses in vivo.Colon Cancer Phase 2 Clinical (In Vitro) :LGK974 effectively displaces [3H]-GNF-1331 with an IC50 of 1 nM in the PORCN radioligand binding assay. LGK974 potently reduces Wnt-dependent AXIN2 mRNA levels in HN30 cells with an IC50 of 0.3 nM. (In Vivo) :LGK974, a drug that targets Porcupine, a Wnt-specific acyltransferase. LGK974 potently inhibits Wnt signaling, has strong efficacy in rodent tumor models, and is well-tolerated. Toxicology studies are performed on nontumor bearing rats at 3 and 20 mg/kg. At the efficacious dose of 3 mg/kg per day for 14 d, LGK974 is well-tolerated without abnormal histopathological findings in Wnt-dependent tissues, including the intestine, stomach, and skin. When rats are administrated a very high dose of 20 mg/kg per day for 14 d, loss of intestinal epithelium is observed, consistent with the concept that Wnt is required for intestinal tissue homeostasis.
CAS Number
1243244-14-5
Product Name Alternative
LGK-974 | LGK974 | LGK 974 | WNT 974 | WNT974
Field of Research
Stem Cell & Developmental Biology
Purity
>98% (HPLC)
Solubility
DMSO: ≥ 32 mg/mL
Smiles
O=C (NC1=NC=C (C2=NC=CN=C2) C=C1) CC3=CN=C (C4=CC (C) =NC=C4) C (C) =C3
Molecular Formula
C23H20N6O
Molecular Weight
396.4445
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
[2,4'-Bipyridine]-5-acetamide, 2',3-dimethyl-N-[5- (2-pyrazinyl) -2-pyridinyl]-

Chemical Information

Wnt-974

LGK974 is a carboxamide, the structure of which is that of acetamide substituted on carbon by a 2',3-dimethyl-2,4'-bipyridin-5-yl group and on nitrogen by a 5-(pyrazin-2-yl)pyridin-2-yl group. It is a highly potent, selective and orally bioavailable Porcupine inhibitor (a Wnt signalling inhibitor). It has a role as a Wnt signalling inhibitor. It is a secondary carboxamide, a member of pyridines, a member of pyrazines and a member of bipyridines. It is functionally related to an acetamide.

CAS Number1243244-14-5
PubChem CID46926973
IUPAC Name2-[5-methyl-6-(2-methyl-4-pyridinyl)-3-pyridinyl]-N-(5-pyrazin-2-yl-2-pyridinyl)acetamide
Molecular FormulaC23H20N6O
Molecular Weight396.4
XLogP1.8
Topological Polar Surface Area93.6
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count6
Rotatable Bond Count5
Heavy Atom Count30
Formal Charge0
Complexity560
SMILES
CC1=CC(=CN=C1C2=CC(=NC=C2)C)CC(=O)NC3=NC=C(C=C3)C4=NC=CN=C4
InChI
InChI=1S/C23H20N6O/c1-15-9-17(12-28-23(15)18-5-6-25-16(2)10-18)11-22(30)29-21-4-3-19(13-27-21)20-14-24-7-8-26-20/h3-10,12-14H,11H2,1-2H3,(H,27,29,30)
InChIKey
XXYGTCZJJLTAGH-UHFFFAOYSA-N
Chemical Structure
2D Structure
2D structure of Wnt-974
CAS: 1243244-14-5
CID: 46926973
Formula: C23H20N6O
MW: 396.4
Interactive 3D Structure
Loading 3D structure...
View on PubChemRaw 3D data
Computed Properties
PropertyValue
Molecular Weight396.4
XLogP31.8
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count6
Rotatable Bond Count5
Exact Mass396.16985928
Monoisotopic Mass396.16985928
Topological Polar Surface Area93.6 Ų
Heavy Atom Count30
Formal Charge0
Complexity560
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count1
Compound Is CanonicalizedYes

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