2. Protein Tyrosine Kinase/RTK
  3. c-Kit
  4. AZD3229

AZD3229 is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors. AZD3229 inhibits c-KIT with an IC50 value of 223.3 nM.

For research use only. We do not sell to patients.

AZD3229 Chemical Structure

AZD3229 Chemical Structure

CAS No. : 2248003-60-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 204 In-stock
Solution
10 mM * 1 mL in DMSO USD 204 In-stock
Solid
5 mg USD 185 In-stock
10 mg USD 290 In-stock
25 mg USD 530 In-stock
50 mg USD 880 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of AZD3229:

AZD3229 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

AZD3229 is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors. AZD3229 inhibits c-KIT with an IC50 value of 223.3 nM[1][2].

IC50 & Target

IC50: 223.3 nM (c-Kit)[2]
Cellular Effect
Cell Line Type Value Description References
BaF3 GI50
> 10 μM
Compound: 44; AZD3229
Cytotoxicity in mouse parental BA/F3 cells incubated for 72 hrs by MTS assay
Cytotoxicity in mouse parental BA/F3 cells incubated for 72 hrs by MTS assay
[PMID: 30204441]
In Vitro

AZD3229 is a potent, pan-KIT mutant inhibitor with potent single digit nM growth inhibition against a diverse panel of mutant KIT driven Ba/F3 cell lines (GI50=1-50 nM)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

AZD3229 Related Antibodies
Molecular Weight

479.51

Formula

C24H26FN7O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

COCCOC1=CC(F)=C2C(N=CN=C2NC3=CC=C(NC(CN4C=C(C(C)C)N=N4)=O)C=C3)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 40 mg/mL (83.42 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 2.0855 mL 10.4273 mL 20.8546 mL
5 mM 0.4171 mL 2.0855 mL 4.1709 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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: 4 mg/mL (8.34 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 4 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (40.0 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% (20% SBE-β-CD in Saline)

    Solubility: 4 mg/mL (8.34 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 4 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (40.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0855 mL 10.4273 mL 20.8546 mL 52.1366 mL
5 mM 0.4171 mL 2.0855 mL 4.1709 mL 10.4273 mL
10 mM 0.2085 mL 1.0427 mL 2.0855 mL 5.2137 mL
15 mM 0.1390 mL 0.6952 mL 1.3903 mL 3.4758 mL
20 mM 0.1043 mL 0.5214 mL 1.0427 mL 2.6068 mL
25 mM 0.0834 mL 0.4171 mL 0.8342 mL 2.0855 mL
30 mM 0.0695 mL 0.3476 mL 0.6952 mL 1.7379 mL
40 mM 0.0521 mL 0.2607 mL 0.5214 mL 1.3034 mL
50 mM 0.0417 mL 0.2085 mL 0.4171 mL 1.0427 mL
60 mM 0.0348 mL 0.1738 mL 0.3476 mL 0.8689 mL
80 mM 0.0261 mL 0.1303 mL 0.2607 mL 0.6517 mL
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AZD3229 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:

AZD32292248003-60-1AZD 3229AZD-3229c-KitSCFRCD117Inhibitorinhibitorinhibit

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