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Article

D-1553: A novel KRASG12C inhibitor with potent and selective cellular and in vivo antitumor activity.

Cancer science - 1 Jul 2023

Shi Zhe, Weng Jifang, Niu Haotao, Yang Hong, Liu Rongfeng, Weng Yan, Zhu Qingqing, Zhang Yihong, Tao Liangshan, Wang Zhenwu, Huh Seok Jae, Jiang Yueheng, Mei Hong, Dai Xing, Zhang Ling, Wang Yaolin

Abstract excerpt

D-1553 is a small molecule inhibitor selectively targeting KRASG12C and currently in phase II clinical trials. Here, we report the preclinical data demonstrating antitumor activity of D-1553. Potency and specificity of D-1553 in inhibiting GDP-bound KRASG12C mutation were determined by thermal shift assay and KRASG12C -coupled nucleotide exchange assay. In vitro and in vivo antitumor activity of D-1553 alone or...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Identifiers

PMID: 37158138
DOI: 10.1111/cas.15829
PMCID: PMC10323112

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