LGK974 (WNT974; LGK974)
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 100mg | $850 | In Stock |
| 250mg | $1550 | In Stock |
| 500mg | $2325 | In Stock |
: Cat #: V1353 CAS #: 1243244-14-5 Purity ≥ 98%
Description: LGK-974 (formerly known as WNT-974; LGK-974 and NVP-LGK974) is a novel potent, orally bioavailable and specific/selective PORCN (Porcupine) inhibitor with potential anticancer activity.
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- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 396.44 |
|---|---|
| Molecular Formula | C23H20N6O |
| CAS No. | 1243244-14-5 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 79 mg/mL (199.3 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: <1 mg/mL | |
| Solubility In Vivo | 2% DMSO+corn oil: 5 mg/mL |
| Synonyms | NVP-LGK974; NVPLGK974; NVP LGK974; LGK974; LGK-974; LGK 974; WNT974; WNT 974; WNT-974 Chemical Name: 2-(2',3-dimethyl-[2,4'-bipyridin]-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide SMILES Code: O=C(NC1=NC=C(C2=NC=CN=C2)C=C1)CC3=CN=C(C4=CC(C)=NC=C4)C(C)=C3 Exact Mass: 396.16986 |
| Protocol | In Vitro | In the PORCN radioligand binding assay, LGK974 effectively replaces [3H]-GNF-1331，IC50 is 1 nM. LGK974 effectively reduces Wnt-dependent AXIN30 mRNA levels in HN2 cells, IC50 is 0.3 nM |
|---|---|---|
| In Vivo | LGK974, a drug that targets Porcupine, a Wnt-specific acyltransferase. LGK974 effectively inhibits Wnt signaling, has a strong efficacy in rodent tumor models, and is well tolerated. Toxicological studies were performed on 3 and 20 mg/kg non-tumor-bearing rats. LGK3 was well tolerated at an effective dose of 14 mg/kg daily for 974 days, with no abnormal histopathological findings in Wnt-dependent tissues, including intestine, stomach, and skin. Intestinal epithelial cell loss was observed when rats were administered at very high doses of 20 mg/kg per day for 14 days, consistent with the concept that Wnt is necessary for intestinal tissue homeostasis |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.5224 mL | 12.6122 mL | 25.2245 mL | 50.4490 mL |
| 5mM | 0.5045 mL | 2.5224 mL | 5.0449 mL | 10.0898 mL |
| 10mM | 0.2522 mL | 1.2612 mL | 2.5224 mL | 5.0449 mL |
| 20mM | 0.1261 mL | 0.6306 mL | 1.2612 mL | 2.5224 mL |
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
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Volume
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Molecular Weight*
The dilution calculator equation
Concentration(start)
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Volume(start)
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This equation is commonly abbreviated as: C1 V1 = C2 V2
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V1
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Step One: Enter information below
Dosage mg/kg
Average weight of animals g
Dosing volume per animal µL
Number of animals
Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
mg/ml;
Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
DMSO(Master liquid concentration
mg/mL)
,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.