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LLY-283

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Catalog No. T15767Cas No. 2040291-27-6

LLY-283 is a potent, selective, and oral protein arginine methyltransferase 5 (PRMT5) inhibitor, exhibiting an IC50 of 22 nM and a Kd of 6 nM for the PRMT5:MEP50 complex, and demonstrates antitumor activity.

LLY-283

LLY-283

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🥰Excellent
Purity: 99.22%
Catalog No. T15767Cas No. 2040291-27-6
LLY-283 is a potent, selective, and oral protein arginine methyltransferase 5 (PRMT5) inhibitor, exhibiting an IC50 of 22 nM and a Kd of 6 nM for the PRMT5:MEP50 complex, and demonstrates antitumor activity.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$34In StockIn Stock
5 mg$79In StockIn Stock
10 mgPreferentialIn StockIn Stock
50 mgPreferentialIn StockIn Stock
1 mL x 10 mM (in DMSO)$88In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.22%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
LLY-283 is a potent, selective, and oral protein arginine methyltransferase 5 (PRMT5) inhibitor, exhibiting an IC50 of 22 nM and a Kd of 6 nM for the PRMT5:MEP50 complex, and demonstrates antitumor activity.
Targets&IC50
PRMT5:(ki)6 nM, PRMT5:22 nM, MEP50:22 nM, MEP50:(ki)6 nM
In vitro
LLY-283 is a potent, oral, and selective arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 22 nM in vitro and 25 nM in cells, and a Kd of 6 nM for the PRMT5:MEP50 complex in vitro; LLY-283 inhibits A375 cell proliferation with an IC50 of 46 nM[1].
In vivo
LLY-283 administered orally at a dose of 20 mg/kg daily significantly inhibits tumor growth in A375 cell-bearing mice over a 28-day treatment period[1].
Chemical Properties
Molecular Weight342.35
FormulaC17H18N4O4
Cas No.2040291-27-6
Smiles[H][C@@]1(O[C@H]([C@H](O)[C@@H]1O)n1ccc2c(N)ncnc12)[C@H](O)c1ccccc1
Relative Density.no data available
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
H2O: 3.57 mg/mL (10.43 mM), Sonication and heating to 60℃ are recommended.
DMSO: 112.5 mg/mL (328.61 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (11.68 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
H2O/DMSO
1mg5mg10mg50mg
1 mM2.9210 mL14.6049 mL29.2099 mL146.0494 mL
5 mM0.5842 mL2.9210 mL5.8420 mL29.2099 mL
10 mM0.2921 mL1.4605 mL2.9210 mL14.6049 mL
DMSO
1mg5mg10mg50mg
20 mM0.1460 mL0.7302 mL1.4605 mL7.3025 mL
50 mM0.0584 mL0.2921 mL0.5842 mL2.9210 mL
100 mM0.0292 mL0.1460 mL0.2921 mL1.4605 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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