2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. AZD0022

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.

AZD0022

AZD0022 Chemical Structure

CAS No. : 2958627-18-2

Size Price Stock Quantity
1 mg In-stock
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of AZD0022:

AZD0022 Related Antibodies

Top Publications Citing Use of Products

View All Ras Isoform Specific Products:

View All Isoforms
K-Ras H-Ras N-Ras Ras

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

AZD0022 is a selective and orally active KRASG12D inhibitor. AZD0022 inhibits KRAS pathway suppression in the GP2D xenograft model[1].

IC50 & Target[1]

KRas G12D

 

In Vivo

Blood clearance of AZD0022 was 8.2 and 8.6 mL/min/kg in mice and dogs, respectively[1].
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.
Clinical Trial
Molecular Weight

614.64

Formula

C34H30F4N6O
CAS No.
Appearance

Solid

Color

Off-white to light yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6270 mL 8.1348 mL 16.2697 mL
5 mM 0.3254 mL 1.6270 mL 3.2539 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.07 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
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
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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

AZD0022 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AZD00222958627-18-2AZD 0022AZD-0022RasKRASG12D inhibitorInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
AZD0022
Cat. No.:
HY-173637
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

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) Portuguese - PT (251 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.