Zhengping Wang
A5018750887- Cancer, Hypoxia, and Metabolism
- Cancer Research and Treatments
- Mechanisms of cancer metastasis
- ATP Synthase and ATPases Research
- Biochemical and Molecular Research
- Pancreatic and Hepatic Oncology Research
- Cancer Genomics and Diagnostics
- Medical Research and Treatments
- Cancer-related Molecular Pathways
- Cancer Mechanisms and Therapy
- Protein Degradation and Inhibitors
- Evaluation Methods in Various Fields
- Educational Reforms and Innovations
Revolution Medicines (United States)
2024
Abstract RAS-driven cancers comprise up to 30% of human cancers. RMC-6236 is a RAS(ON) multi-selective noncovalent inhibitor the active, GTP-bound state both mutant and wild-type variants canonical RAS isoforms with broad therapeutic potential for aforementioned unmet medical need. exhibited potent anticancer activity across RAS-addicted cell lines, particularly those harboring mutations at codon 12 KRAS. Notably, oral administration was tolerated in vivo drove profound tumor regressions...
<p>Supplementary Figure 1 shows RMC-6236 crystal structure in tri-complex, as well biophysical and cellular potencies of by genotype. Supplementary 2 demonstrates dose-dependent anti-tumor activities at tolerable doses; pharmacodynamic effects on RAS signaling NCI-H441 xenograft tumors assessed IHC, relatively refractory KP-4 NCI-H2122 human DUSP6 mRNA expression vivo. 3 genotype dependent response across NSCLC, PDAC CRC; potential modifiers to the durability KRASG12C NSCLC models upon...
<p>RMC-6236 synthetic route and detailed PK/PD/Efficacy Modeling method</p>
<p>Supplementary Figure 1 shows RMC-6236 crystal structure in tri-complex, as well biophysical and cellular potencies of by genotype. Supplementary 2 demonstrates dose-dependent anti-tumor activities at tolerable doses; pharmacodynamic effects on RAS signaling NCI-H441 xenograft tumors assessed IHC, relatively refractory KP-4 NCI-H2122 human DUSP6 mRNA expression vivo. 3 genotype dependent response across NSCLC, PDAC CRC; potential modifiers to the durability KRASG12C NSCLC models upon...
<p>Supplementary Figure 1 shows RMC-6236 crystal structure in tri-complex, as well biophysical and cellular potencies of by genotype. Supplementary 2 demonstrates dose-dependent anti-tumor activities at tolerable doses; pharmacodynamic effects on RAS signaling NCI-H441 xenograft tumors assessed IHC, relatively refractory KP-4 NCI-H2122 human DUSP6 mRNA expression vivo. 3 genotype dependent response across NSCLC, PDAC CRC; potential modifiers to the durability KRASG12C NSCLC models upon...
<p>RMC-6236 synthetic route and detailed PK/PD/Efficacy Modeling method</p>
<div>Abstract<p>RAS-driven cancers comprise up to 30% of human cancers. RMC-6236 is a RAS(ON) multi-selective noncovalent inhibitor the active, GTP-bound state both mutant and wild-type variants canonical RAS isoforms with broad therapeutic potential for aforementioned unmet medical need. exhibited potent anticancer activity across RAS-addicted cell lines, particularly those harboring mutations at codon 12 <i>KRAS</i>. Notably, oral administration was tolerated...
<div>Abstract<p>RAS-driven cancers comprise up to 30% of human cancers. RMC-6236 is a RAS(ON) multi-selective noncovalent inhibitor the active, GTP-bound state both mutant and wild-type variants canonical RAS isoforms with broad therapeutic potential for aforementioned unmet medical need. exhibited potent anticancer activity across RAS-addicted cell lines, particularly those harboring mutations at codon 12 <i>KRAS</i>. Notably, oral administration was tolerated...