An inhibitor of c-Kit-driven cell proliferation

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Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

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Product Categories

Product Type

Biochemicals

Research Area

Cancer

Cell Signaling

Growth Factor Receptor Signaling

AZD 3229

Name: AZD 3229
Brand: -

Item No. 27908

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)

Technical Information

Formal Name

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

CAS Number

2248003-60-1

Molecular Formula

C₂₄H₂₆FN₇O₃

Formula Weight

479.5

Purity

≥98%

Formulation (Request formulation change)

A crystalline solid

Solubility(Learn about Variance in Solubility)

DMF: 10 mg/mlDMSO: 10 mg/mlEthanol: 0.3 mg/mlPBS (pH 7.2): Partially soluble

λ_max

219, 235, 263, 312 nm

SMILES

COCCOC1=CC(F)=C(C(NC2=CC=C(NC(CN3N=NC(C(C)C)=C3)=O)C=C2)=NC=N4)C4=C1

InChi Code

InChI=1S/C24H26FN7O3/c1-15(2)21-12-32(31-30-21)13-22(33)28-16-4-6-17(7-5-16)29-24-23-19(25)10-18(35-9-8-34-3)11-20(23)26-14-27-24/h4-7,10-12,14-15H,8-9,13H2,1-3H3,(H,28,33)(H,26,27,29)

InChi Key

FLJOFQUXYAWOPE-UHFFFAOYSA-N

Shipping & Storage Information

Storage

-20°C

Shipping

Room temperature in continental US; may vary elsewhere

Certificates of Analysis & Batch Specific Data

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500 µg

$75

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1 mg

$143

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5 mg

$315

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Product Description

AZD 3229 is an inhibitor of c-Kit-driven cell proliferation.¹ It selectively inhibits growth of c-Kit mutant (GI₅₀s = 1-971 nM) and PDGFR mutant (GI₅₀s = 1-22 nM) Ba/F3 cell lines over Ba/F3 cell lines expressing Tel-KDR/VEGFR2 (GI₅₀ = 1,378 nM). AZD 3229 (20 mg/kg twice per day) induces tumor regression in a Ba/F3 mouse xenograft model and a mouse allograft model using Ba/F3 cells expressing KIT-exon 11 del/V654A, a common mutation in gastrointestinal stromal tumors (GIST).

WARNING This product is not for human or veterinary use.

References & Product Citations

Product Description References

1. Kettle, J.G., Anium, R., Barry, E., 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 tumor. J. Med. Chem. 61(19), 8797-8810 (2018).

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