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Opnurasib

🥰Excellent
Catalog No. T40292Cas No. 2653994-08-0
Alias Opnurasib, NVP-JDQ443, JDQ-443

Opnurasib (JDQ-443) is an orally available and selective and potent covalent KRAS G12C inhibitor with antitumor activity for the study of advanced non-small cell lung cancer.

Opnurasib

Opnurasib

🥰Excellent
Purity: 98.88%
Catalog No. T40292Alias Opnurasib, NVP-JDQ443, JDQ-443Cas No. 2653994-08-0
Opnurasib (JDQ-443) is an orally available and selective and potent covalent KRAS G12C inhibitor with antitumor activity for the study of advanced non-small cell lung cancer.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$107In StockIn Stock
5 mg$372In StockIn Stock
10 mg$555In StockIn Stock
25 mg$893In StockIn Stock
50 mgPreferentialIn StockIn Stock
1 mL x 10 mM (in DMSO)$428In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:98.88%
Appearance:Solid
Color:White to Yellow
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Product Introduction

Bioactivity
Description
Opnurasib (JDQ-443) is an orally available and selective and potent covalent KRAS G12C inhibitor with antitumor activity for the study of advanced non-small cell lung cancer.
In vitro
Opnurasib selectively forms a covalent bond with and inhibits GDP-bound KRASG12C, demonstrating a low reversible binding affinity to the RAS switch II pocket. Additionally, it effectively hinders the proliferation of cell lines carrying KRASG12C mutations, as well as those with double mutations G12C/H95, G12C/R68S, and G12C/Y96.[2]
Opnurasib induces dose-dependent decreases in phosphorylated ERK (pERK) levels and inhibits the proliferation of KRASG12C-mutated cell lines NCI-H358 and NCI-H2122, exhibiting IC50 values of 0.018 and 0.063 μM, respectively.[2]
In vivo
Opnurasib elicits distinct antitumor responses in patient-derived xenograft (PDX) models of non-small cell lung cancer (NSCLC) and colorectal tumors, and these responses are further enhanced when Opnurasib is used in combination with other therapeutic agents.[2]
SynonymsOpnurasib, NVP-JDQ443, JDQ-443
Chemical Properties
Molecular Weight526.03
FormulaC29H28ClN7O
Cas No.2653994-08-0
SmilesCc1c(c(nn1C1CC2(C1)CN(C2)C(=O)C=C)-c1ccc2n(C)ncc2c1)-c1c(Cl)c(C)cc2[nH]ncc12
Relative Density.1.46 g/cm3 (Predicted)
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
DMSO: 70 mg/mL (133.07 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (6.27 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
DMSO
1mg5mg10mg50mg
1 mM1.9010 mL9.5052 mL19.0103 mL95.0516 mL
5 mM0.3802 mL1.9010 mL3.8021 mL19.0103 mL
10 mM0.1901 mL0.9505 mL1.9010 mL9.5052 mL
20 mM0.0951 mL0.4753 mL0.9505 mL4.7526 mL
50 mM0.0380 mL0.1901 mL0.3802 mL1.9010 mL
100 mM0.0190 mL0.0951 mL0.1901 mL0.9505 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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μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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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

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