自学自救 发表于 2025-4-8 10:50:34

完全可以合理推论,阿扎胞苷对kras g12c的疗效不会比Sotorasib差

1、《Computational insights into KRAS G12C inhibition: exploring possible repurposing of Azacitidine and Ribavirin》
“Azacitidine and Ribavirin, exhibited substantial binding affinities of -8.7 and -8.3 kcal/mol, respectively.”
阿扎胞苷、利巴韦林对 kras g12c 的结合亲和力是 -8.7 and -8.3 kcal/mol。

2、《Establishing the Role of Iridoids as Potential Kirsten Rat Sarcoma Viral Oncogene Homolog G12C Inhibitors Using Molecular Docking; Molecular Docking Simulation; Molecular Mechanics Poisson-Boltzmann Surface Area; Frontier Molecular Orbital Theory; Molecular Electrostatic Potential; and Absorption, Distribution, Metabolism, Excretion, and Toxicity Analysis》
Sotorasib (dock score: -9.1 kcal/mol).
kras g12c 已经上市的靶向药 Sotorasib 跟kras g12c的结合亲和力是 -9.1 kcal/mol.

3、阿扎胞苷只比 Sotorasib 低一点点;但是阿扎胞苷注射药 ,皮下注射给药为主,也有静脉给药的用法;Sotorasib是口服药;阿扎胞苷的生物利用度比Sotorasib要高很多;因此完全可以合理推论,阿扎胞苷对kras g12c的疗效不会比Sotorasib差。
阿扎胞苷分子量很小只有 244.2,也不用担心不入脑的问题。
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