Catalog No.S7143 Synonyms: NVP-LGK974
Molecular Weight(MW): 396.44
LGK-974 is a potent and specific PORCN inhibitor, and inhibits Wnt signaling with IC50 of 0.4 nM in TM3 cells. Phase 1.
2 Customer Reviews
AP1/Jun noncanonical Wnt activity measured in the presence of LGK974 (porcupine inhibitor) and JNK-IN-8 (JNK inhibitor) (both 1 μM). F: Aldosterone secretion during the same experiment (n=4). Results are expressed in mean SEM, and P values show significance between treatments and baseline control.
J Clin Endocrinol Metab, 2015, 100(6): E836-44. LGK-974 purchased from Selleck.
Nestin silencing inhibits the Wnt/β-catenin signaling in breast CSC. Nestin-si and Nestin-c breast CSC were cultured for 48 h, and the relative levels of target proteins and phosphorylation were determined by western blotting. Data are presented as the mean ± SD of the levels of target proteins vs. the β-actin control, or the phosphorylated vs. the total form, from six separate experiments. In addition, Nestinhigh in the presence or absence of LGK974 (1 nM), Nestinlow in the presence or absence of SB216763 (5 uM), and control CSC were tested for their proliferation via mammosphere formation assays. Quantitative analysis of the formed mammospheres. *P <0.05, vs. the Nestin-c or control, except for specifically indicated. CSC, cancer stem cell; SD, standard deviation.
Breast Cancer Res 2014 16(4), 408. LGK-974 purchased from Selleck.
Purity & Quality Control
Choose Selective Wnt/beta-catenin Inhibitors
|Description||LGK-974 is a potent and specific PORCN inhibitor, and inhibits Wnt signaling with IC50 of 0.4 nM in TM3 cells. Phase 1.|
|Features||Orally bioavailable Porcupine-specific inhibitor that has been tested in Phase I clinical trials for treatment of malignancies dependent on Wnt ligands.|
LGK974 effectively displaces [3H]-GNF-1331 with IC50 of 1 nM in the PORCN radioligand binding assay, and shows no major cytotoxicity in cells up to 20 µM. LGK974 shows comparable inhibitory activities against all tested Wnts with IC50 ranging from 0.05 to 2.4 nM, which is consistent with the genetic loss of PORCN phenotype.  LGK974 specifically inhibits the growth of three RNF43-mutant cell lines, HPAF-II, PaTu 8988S, and Capan-2. 
|In vivo||In a murine MMTV-Wnt1 tumor model and a human head and neck squamous cell carcinoma model (HN30), LGK974 (3 mg/kg) inhibits Wnt signaling in vivo and induces tumor regression without significant body weight loss in the mice.  LGK974 (5 mg/kg, p.o., BID) also inhibits tumor growth of RNF43-mutant pancreatic tumors (HPAF-II and Capan-2) in vivo. |
|In vitro||DMSO||79 mg/mL warmed (199.27 mM)|
|In vivo||Add solvents individually and in order:
2% DMSO+corn oil
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01351103||Suspended||Pancreatic Adenocarcinoma|BRAF Mutant Colorectal Cancer|Other Tumor Types With Documented Genetic Alterations Upstream in the Wnt Signaling Pathway||Novartis Pharmaceuticals|Novartis||December 2011||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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Frequently Asked Questions
If LGK974 is a lipophilic or hydrophilic substance?
LGK974 is a lipophilic compound.