AZD0022
Based on 1 Customer Validation
AZD0022 is a selective and orally active KRASG12D inhibitor. AZD0022 inhibits KRAS pathway suppression in the GP2D xenograft model.
For research use only. We do not sell to patients.
- Purity: 98.36%
- CAS No.: 2958627-18-2
- Formula: C34H30F4N6O
- Molecular Weight:614.64
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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KRas G12D |
In the GP2D model, single oral 150 mg/kg doses displays prolonged plasma and tumour exposure. AZD0022 is estimated to be 18x more bound in tumour tissue than in plasma. Seven days of continuous 150mg/kg BID dosing resulted in up to approx. 75% pRSK inhibition. A dose range of 10, 50 and 150 mg/kg BID over 7 days display exposure-dependent pRSK modulation, with maximal of 75% pRSK inhibition[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2958627-18-2
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Appearance Solid
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Molecular Weight 614.64
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Formula C34H30F4N6O
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Color Off-white to light yellow
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SMILES
FC1=C(C#C)C2=[C@]([C@]3=C(F)C(N=C(OC[C@]4(C[C@@H](F)C5)N5CCC4)N=C6N7C[C@H]8N[C@H](C=C8)C7)=C6C=C3F)C=C(N)C=C2C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (162.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.07 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.6270 mL | 8.1348 mL | 16.2697 mL | 40.6742 mL |
| 5 mM | 0.3254 mL | 1.6270 mL | 3.2539 mL | 8.1348 mL | |
| 10 mM | 0.1627 mL | 0.8135 mL | 1.6270 mL | 4.0674 mL | |
| 15 mM | 0.1085 mL | 0.5423 mL | 1.0846 mL | 2.7116 mL | |
| 20 mM | 0.0813 mL | 0.4067 mL | 0.8135 mL | 2.0337 mL | |
| 25 mM | 0.0651 mL | 0.3254 mL | 0.6508 mL | 1.6270 mL | |
| 30 mM | 0.0542 mL | 0.2712 mL | 0.5423 mL | 1.3558 mL | |
| 40 mM | 0.0407 mL | 0.2034 mL | 0.4067 mL | 1.0169 mL | |
| 50 mM | 0.0325 mL | 0.1627 mL | 0.3254 mL | 0.8135 mL | |
| 60 mM | 0.0271 mL | 0.1356 mL | 0.2712 mL | 0.6779 mL | |
| 80 mM | 0.0203 mL | 0.1017 mL | 0.2034 mL | 0.5084 mL | |
| 100 mM | 0.0163 mL | 0.0813 mL | 0.1627 mL | 0.4067 mL |
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