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AZD0022

🥰Excellent
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

🥰Excellent
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]
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Purity:98.73%
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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
ColorYellow
AppearanceSolid
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.
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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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2OTargetMol | reagent mix well and clarify
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