[CAS NO. 2248003-71-4] AZD3229Tosylate

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Catalog:	HY-112802A
Brand:	MCE
CAS:	2248003-71-4

Overview

MDL	-
Molecular Weight	651.71
Molecular Formula	C31H34FN7O6S
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

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

Summary

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 (GI ₅₀ =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] .

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

Appearance

Solid

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 )

* "≥" 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
10 mM	0.1534 mL	0.7672 mL	1.5344 mL

* Please refer to the solubility information to select the appropriate solvent.

References

[1] Kettle JG, et al. Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. J Med Ch

Synonyms

1H-1,2,3-Triazole-1-acetamide, N-[4-[[5-fluoro-7-(2-methoxyethoxy)-4-quinazolinyl]amino]phenyl]-4-(1-methylethyl)-, 4-methylbenzenesulfonate (1:1)

N-(4-[[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino]phenyl)-2-[4-(propan-2-yl)-1H-[1,2,3]triazol-1-yl]acetamide tosylate

AZD 3229 tosylate

AZD3229 tosylate

AZD-3229 tosylate

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