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AZD0022

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Catalog No. T204084Cas No. 2958627-18-2
Alias AZD 0022

AZD0022 is a selective, reversible, and orally active KRAS G12D inhibitor exhibiting high affinity for both active (KRAS G12D-GTP) and inactive (KRAS G12D-GDP) proteins, whilst demonstrating selectivity for wild-type KRAS. AZD0022 exhibits tumour marker inhibition in PDAC and NSCLC models, making it suitable for investigating tumours such as advanced solid tumours, pancreatic cancer, and colorectal cancer.

AZD0022

AZD0022

😃Good
Purity: 98.73%
Catalog No. T204084Alias AZD 0022Cas No. 2958627-18-2
AZD0022 is a selective, reversible, and orally active KRAS G12D inhibitor exhibiting high affinity for both active (KRAS G12D-GTP) and inactive (KRAS G12D-GDP) proteins, whilst demonstrating selectivity for wild-type KRAS. AZD0022 exhibits tumour marker inhibition in PDAC and NSCLC models, making it suitable for investigating tumours such as advanced solid tumours, pancreatic cancer, and colorectal cancer.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$679-In Stock
5 mg$1,490-In Stock
10 mg$2,530-In Stock
25 mg$4,950-In Stock
1 mL x 10 mM (in DMSO)$2,130-In 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:98.73%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
AZD0022 is a selective, reversible, and orally active KRAS G12D inhibitor exhibiting high affinity for both active (KRAS G12D-GTP) and inactive (KRAS G12D-GDP) proteins, whilst demonstrating selectivity for wild-type KRAS. AZD0022 exhibits tumour marker inhibition in PDAC and NSCLC models, making it suitable for investigating tumours such as advanced solid tumours, pancreatic cancer, and colorectal cancer.
In vitro
PKPD modelling of AZD0022 suggested an unbound IC50 of 1.4 nM for pRSK inhibition[1].
In vivo
In nude mice bearing GP2D human tumor xenografts, oral dosing of AZD0022 at 150 mg/kg led to sustained plasma and tumor exposure, with tumor concentrations approximately 18-fold higher than plasma. Seven days of BID dosing at 150 mg/kg resulted in up to 75% inhibition of pRSK, with dose-dependent target modulation observed across 10, 50, and 150 mg/kg[1].
SynonymsAZD 0022
Chemical Properties
Molecular Weight614.64
FormulaC34H30F4N6O
Cas No.2958627-18-2
SmilesFC=1C=CC2=CC(N)=CC(C=3C(F)=CC=4C(=NC(=NC4N5CC6C=CC(N6)C5)OCC78N(CCC7)CC(F)C8)C3F)=C2C1C#C
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 80 mg/mL (130.16 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (5.37 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 mM1.6270 mL8.1348 mL16.2697 mL81.3484 mL
5 mM0.3254 mL1.6270 mL3.2539 mL16.2697 mL
10 mM0.1627 mL0.8135 mL1.6270 mL8.1348 mL
20 mM0.0813 mL0.4067 mL0.8135 mL4.0674 mL
50 mM0.0325 mL0.1627 mL0.3254 mL1.6270 mL
100 mM0.0163 mL0.0813 mL0.1627 mL0.8135 mL

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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
%
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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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