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

AZD3229 Tosylate is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors.

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

AZD3229 Tosylate Chemical Structure

AZD3229 Tosylate Chemical Structure

CAS No. : 2248003-71-4

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Based on 1 publication(s) in Google Scholar

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Description

AZD3229 Tosylate is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors.

IC50 & Target

KIT[1].

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). AZD3229 demonstrates potent single digit nM growth inhibition across a broad cell panel, with good margin to KDR-driven effects. Selectivity over KDR can be rationalised predominantly by the interaction of water molecules with the protein and ligand in the active site and its kinome selectivity is similar to the best of the approved GIST agents[1].

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

Molecular Weight

651.71

Formula

C31H34FN7O6S

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

COCCOC1=CC(F)=C2C(N=CN=C2NC3=CC=C(NC(CN4C=C(C(C)C)N=N4)=O)C=C3)=C1.CC5=CC=C(S(O)(=O)=O)C=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (153.44 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5344 mL 7.6721 mL 15.3442 mL
5 mM 0.3069 mL 1.5344 mL 3.0688 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

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

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
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 (sealed storage, away from moisture). 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 1.5344 mL 7.6721 mL 15.3442 mL 38.3606 mL
5 mM 0.3069 mL 1.5344 mL 3.0688 mL 7.6721 mL
10 mM 0.1534 mL 0.7672 mL 1.5344 mL 3.8361 mL
15 mM 0.1023 mL 0.5115 mL 1.0229 mL 2.5574 mL
20 mM 0.0767 mL 0.3836 mL 0.7672 mL 1.9180 mL
25 mM 0.0614 mL 0.3069 mL 0.6138 mL 1.5344 mL
30 mM 0.0511 mL 0.2557 mL 0.5115 mL 1.2787 mL
40 mM 0.0384 mL 0.1918 mL 0.3836 mL 0.9590 mL
50 mM 0.0307 mL 0.1534 mL 0.3069 mL 0.7672 mL
60 mM 0.0256 mL 0.1279 mL 0.2557 mL 0.6393 mL
80 mM 0.0192 mL 0.0959 mL 0.1918 mL 0.4795 mL
100 mM 0.0153 mL 0.0767 mL 0.1534 mL 0.3836 mL
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AZD3229 Tosylate 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.

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Product Name:
AZD3229 Tosylate
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HY-112802A
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