LGK-974

Catalog No. A12816

LGK974是高效，选择性和口服生物利用性的豪猪抑制剂（Wnt信号拮抗剂），在Wnt信号报告基因测定和豪猪结合测定中IC50 <1 nM。

Product Citations

A-Ri Cho, .et al. RNF43 R117fs mutant positively regulates Wnt/β-catenin signaling by failing to internalize FZD expressed on the cell surface, Sci Rep, 2022, Apr 29;12(1):7013 PMID: 35487932
Yang JM, .et al. LGK974, a PORCUPINE inhibitor, mitigates cytotoxicity in an in vitro model of Parkinson's disease by interfering with the WNT/β-CATENIN pathway, Toxicology, 2018, Dec 1;410:65-72 PMID: 30205152
E Lemieux, .et al. Oncogenic KRAS signalling promotes the Wnt/β-catenin pathway through LRP6 in colorectal cancer, Oncogene, 2015, Sep 17; 34(38): 4914-4927 PMID: 25500543

Technical details

Catalog Num	A12816
M. Wt	396.44
Formula	C23H20N6O
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	1243244-14-5
Synonyms	LGK974, LGK 974
SMILES	CC1=C(N=CC(=C1)CC(=O)NC2=NC=C(C=C2)C3=NC=CN=C3)C4=CC(=NC=C4)C

Biological Activity

LGK974是高效，选择性和口服生物利用性的豪猪抑制剂（Wnt信号拮抗剂），在Wnt信号报告基因测定和豪猪结合测定中IC50 <1 nM。

Targets

Porcn (TM3 cells)

Solubility *

In vitro (25°C)	DMSO	Warmed: 76 mg/mL (191.7 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	2% DMSO+corn oil	4 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	25.22 mL	126.12 mL	252.24 mL
0.5 mM	5.04 mL	25.22 mL	50.45 mL
1 mM	2.52 mL	12.61 mL	25.22 mL
5 mM	0.5 mL	2.52 mL	5.04 mL

*The above data is based on the productmolecular weight 396.44. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.