CQ1373 | RET G810 mutations inhibitor | Probechem Biochemicals

Chemical Structure : CQ1373

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CQ1373 (CQ-1373)

货号: PC-24031Not For Human Use, Lab Use Only.

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250 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	546.94
分子式	C25H22ClF3N6O3
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	(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

参考文献

1. Mingjin Xu, et al. Eur J Med Chem. 2025 Mar 15:286:117294.

CQ1373 (CQ-1373)

生物&药学活性

物理化学性质&存储条件

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CQ1373 (CQ-1373)

生物&药学活性

物理化学性质&存储条件

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