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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 Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 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 |
| 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]. |
| Synonyms | AZD 0022 |
| Molecular Weight | 614.64 |
| Formula | C34H30F4N6O |
| Cas No. | 2958627-18-2 |
| Smiles | FC=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 | Powder: -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
| ||||||||||||||||||||||||||||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
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 ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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