K-Ras G12C-IN-2 - CAS 1629267-75-9
Catalog number: 1629267-75-9
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
K-Ras G12C-IN-2 is a novel and irreversible inhibitor of mutant K-ras G12C.
K-Ras G12C-IN-2
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1.K-ras gene mutation as an early prognostic marker of colon cancer.
Szpon Ł, Stal A, Zawadzki M, Lis-Nawara A, Kielan W, Grzebieniak Z. Pol Przegl Chir. 2016 Jan 1;88(1):15-9. doi: 10.1515/pjs-2016-0021.
Due to increased colorectal cancer incidence there is a necessity of seeking new both prognostic and prediction factors that will allow to evolve new diagnostic tests. K-ras gene seems to be such a factor and its mutations are considered to be an early marker of progression of colorectal cancer. The aim of the study was to find a correlation between K-ras gene mutation in patients with diagnosed colorectal cancer and selected clinical parameters.
2.Discordance of Mutation Statuses of Epidermal Growth Factor Receptor and K-ras between Primary Adenocarcinoma of Lung and Brain Metastasis.
Rau KM1,2, Chen HK3, Shiu LY4,5, Chao TL6, Lo YP7, Wang CC8,9, Lin MC10,11, Huang CC12,13. Int J Mol Sci. 2016 Apr 7;17(4). pii: E524. doi: 10.3390/ijms17040524.
Mutations on epidermal growth factor receptor (EGFR) of adenocarcinomas of lung have been found to be associated with increased sensitivity to EGFR tyrosine kinase inhibitors and K-ras mutations may correlate with primary resistance. We aimed to explore the discordant mutation statuses of EGFR and K-ras between primary tumors and matched brain metastases in adenocarcinomas of lung. We used a sensitive Scorpion ARMS method to analyze EGFR mutation, and Sanger sequencing followed by allele-specific real-time polymerase chain reaction to analyze K-ras mutation. Forty-nine paired tissues with both primary adenocarcinoma of lung and matched brain metastasis were collected. Thirteen patients (26.5%) were discordant for the status of EGFR between primary and metastatic sites. K-ras gene could be checked in paired specimens from 33 patients, thirteen patients (39.6%) were discordant for the status of K-ras. In primary lung adenocarcinoma, there were 14 patients of mutant EGFR had mutant K-ras synchronously.
3.Synergistic effects of sorafenib in combination with gemcitabine or pemetrexed in lung cancer cell lines with K-ras mutations.
Li J1, Wang S2, Su ZF2, Yuan Y2. Contemp Oncol (Pozn). 2016;20(1):33-8. doi: 10.5114/wo.2016.58499. Epub 2016 Mar 16.
K-ras is currently accepted as the most frequently mutated oncogene in non-small cell lung cancer (NSCLC, including squamous carcinoma, adenocarcinoma, and large cell carcinoma). NSCLC patients with the K-ras mutation appear to be refractory to the majority of systemic therapies. In the present study, the in vitro antitumor effects and correlated molecular mechanisms of sorafenib combined with gemcitabine or pemetrexed were explored in the K-ras mutation-positive NSCLC A549 cell line. Sorafenib was seen to exhibit dose-dependent growth inhibition in the A549 cells, while sorafenib combined with pemetrexed demonstrated a greater synergism compared with sorafenib combined with gemcitabine. Sorafenib arrested the cell cycle at the G1 phase, while gemcitabine and pemetrexed caused arrest at the S phase. The molecular mechanism of this synergism was due to the downstream signalling pathways, which were efficiently suppressed by sorafenib, therefore increasing the incidence of the entry of the chemotherapeutic drugs into the apoptotic pathways.
4.Equilibrium Thermodynamics and Kinetics of K-Ras Dimerization through an Effector Binding Surface.
Sayyed-Ahmed A, Gorfe AA. J Phys Chem B. 2016 Apr 12. [Epub ahead of print]
Dimer formation is believed to have a substantial impact on regulating K-Ras function. Yet the evidence for dimerization and the molecular details of the process are scant. In this study, we characterize a K-Ras pseudo-C2-symmetric dimerization interface involving the effector interacting β2-strand. We used structure matching and all-atom molecular dynamics (MD) simulations to predict, refine and investigate the stability of this interface. Our MD simulation revealed that β2-dimer is stable and remained relatively close to its initial conformation due to the presence of a number of hydrogen bonds, ionic salt bridges and other favorable contacts. Furthermore, we carried out potential of mean force calculations to determine the relative binding strength of the interface. The results of these calculations indicated that the β2 dimerization interface provides a weak binding free energy in solution and a dissociation constant close to 1 mM. In addition, analyses of Brownian dynamics simulations suggested an association rate of k_on ≈ 〖10〗^5-〖10〗^6 M^(-1) s^(-1).
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CAS 1629267-75-9 K-Ras G12C-IN-2

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