AZD3229 | KIT mutant inhibitor | Probechem Biochemicals

Chemical Structure : AZD3229

CAS No.: 2248003-60-1

AZD3229 (AZD-3229, AZD 3229)

Catalog No.: PC-35661Not For Human Use, Lab Use Only.

AZD3229 (AZD-3229) 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).

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5 mg	$138	In stock
10 mg	$218	In stock
25 mg	$378	In stock
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Biological Activity

AZD3229 (AZD-3229) 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 shows good margin to KDR-driven effects, also inhibits PDGFR mutants (Tel-PDGFRα, Tel-PDGFRβ, V561D/D842V).

AZD3229 inhibits a broad range of primary and imatinib-resistant secondary mutations seen in GIS.

In engineered and GIST-derived cell lines, AZD3229 is 15 to 60 times more potent than imatinib in inhibiting KIT primary mutations and has low nanomolar activity against a wide spectrum of secondary mutations.

AZD3229 causes durable inhibition of KIT signaling in patient-derived xenograft (PDX) models of GIST, leading to tumor regressions at doses that showed no changes in arterial blood pressure (BP) in rat telemetry studies.

AZD3229 has a superior potency and selectivity profile to standard of care (SoC) agents-imatinib, sunitinib, and regorafenib, as well as investigational agents, avapritinib (BLU-285) and ripretinib (DCC-2618).

AZD3229 exhibited effect against a much broader panel of KIT mutant Ba/F3 cell lines expressing a diverse set of clinically relevant primary and secondary mutations (exon 11 +del V654A, exon 11 +del D816H, exon 11 +del T670I, GI50=2-16 nM), including a small panel of PDGFR driven lines relevant in subsets of GIST.

Physicochemical Properties

M.Wt	479.516
Formula	C24H26FN7O3
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	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

References

1. Kettle JG, et al. J Med Chem. 2018 Sep 24. doi: 10.1021/acs.jmedchem.8b00938.
2. Pilla Reddy V, et al. Clin Cancer Res. 2020 Jul 15;26(14):3751-3759.

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AZD3229 (AZD-3229, AZD 3229)

Biological Activity

Physicochemical Properties

References

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