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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Ras-QTX3034
QTX3034

Chemical Structure : QTX3034

CAS No.: 2972625-49-1

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QTX3034 (QTX-3034)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 663.24
分子式 C35H44ClFN8O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
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

参考文献

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

2. Patent WO2024187174 A2 2024-09-12.

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