QTX3034 | KRAS inhibitor | Probechem Biochemicals

Chemical Structure : QTX3034

CAS No.: 2972625-49-1

QTX3034 (QTX-3034)

Catalog No.: PC-28071Not For Human Use, Lab Use Only.

QTX3034 is a potent, highly selective, orally bioavailable allosteric multi-KRAS inhibitor that is efficacious against a broad spectrum of the more common KRASG12D-and KRASG12V-mutated cancers in vitro and in vivo.

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Biological Activity

QTX3034 is a potent, highly selective, orally bioavailable allosteric multi-KRAS inhibitor that is efficacious against a broad spectrum of the more common KRASG12D-and KRASG12V-mutated cancers in vitro and in vivo.
QTX3034 synergized with three different EGFR inhibitors (afatinib, cetuximab, erlotinib) to profoundly inhibit proliferation across multiple KRASG12D, KRASG12V, and KRASWT Amp mutant cell lines with strong ZIP synergy scores (>10).
Combination of QTX3034 and afatinib exhibited a markedly greater inhibitory effect on KRAS-mutant colony formation compared to the respective single agents.
QTX3034 induced a dose-dependent increase in EGFR phosphorylation in the KRASG12D-mutated cell line GP2D, while co-administration with afatinib robustly inhibited this EGFR activation.

Physicochemical Properties

M.Wt	663.24
Formula	C35H44ClFN8O2
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	3-chloro-5-((S)-2'-(((2R,7aS)-2-fluorotetrahydro-1H-pyrrolizin-7a(5H)-yl)methoxy)-6'-methyl-3,4,5',8'-tetrahydro-2H,6'H-spiro[naphthalene-1,7'-pyrido[4,3-d]pyrimidin]-4'-yl)-N,N-dimethyl-5,6,7,8-tetrahydro-4H-pyrazolo[1,5-a][1,4]diazepine-2-carboxamide

References

1. Yang J. Zhang, et al. Mol Cancer Ther (2023) 22 (12_Supplement): LB_C09.

2. Patent WO2024187174 A2 2024-09-12.

QTX3034 (QTX-3034)

Biological Activity

Physicochemical Properties

References

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