Chemical Structure : CQ1373
CAS No.:
CQ1373
(CQ-1373)
Catalog No.: PC-24031Not For Human Use, Lab Use Only.
CQ1373 is a next generation, selective RET inhibitor with IC50 of 3.0, 25.7 and 28.4 nM against BaF3 cells expressing CCDC6-RET, CCDC6-RET-G810C and CCDC6-RET-G810R, respectively, overcomes RET G810 mutations.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
CQ1373 is a next generation, selective RET inhibitor with IC50 of 3.0, 25.7 and 28.4 nM against BaF3 cells expressing CCDC6-RET, CCDC6-RET-G810C and CCDC6-RET-G810R, respectively, overcomes RET G810 mutations.
CQ1373 demonstrates good selectivity toward wild-type RET and solvent front mutants G810C/R with IC50 values of 4.2, 7.1 and 32.4 nM, respectively.
CQ1373 effectively inhibits RET phosphorylation and downstream signaling through SHC.
CQ1373 also induces apoptosis and cell cycle arrest in a dose-dependent manner in BaF3 cells harboring CCDC6-RET, CCDC6-RET-G810C and CCDC6-RET-G810R fusions.
CQ1373 (25 mg/kg, i,p, qd) exhibits promising in vivo anti-tumor efficacy in a CCDC6-RET-G810R mice xenograft model.
Physicochemical Properties
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M.Wt
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546.94
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Formula
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C25H22ClF3N6O3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(E)-1-(2-chloro-4-(2-(4-(5-methoxypyridin-3-yl)-1H-pyrazol-5-yl)vinyl)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea
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References
1. Mingjin Xu, et al. Eur J Med Chem. 2025 Mar 15:286:117294.
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