Journal: iScience

Article Title: Overcoming MET-mediated resistance in oncogene-driven NSCLC

doi: 10.1016/j.isci.2023.107006

Figure Lengend Snippet: MET overexpression causes resistance to osimertinib, sotorasib, poziotinib, and entrectinib (A) The indicated tetON-MET cells were induced with doxycycline for 48 h before lysis. Western blot analysis was performed with the indicated antibodies. (B) Cells were cultured with doxycycline for 24 h before being treated with the respective targeted therapies. Cellular viability was measured six days from treatment onset. Data are represented as mean of n = 3 ± SD.

Article Snippet: entrectinib , Medchemexpress , NA.

Techniques: Over Expression, Lysis, Western Blot, Cell Culture

Journal: iScience

Article Title: Overcoming MET-mediated resistance in oncogene-driven NSCLC

doi: 10.1016/j.isci.2023.107006

Figure Lengend Snippet:

Article Snippet: entrectinib , Medchemexpress , NA.

Techniques: Recombinant, Synthesized, Hybridization, Software

Journal: Cell Reports Medicine

Article Title: Entrectinib inhibits NLRP3 inflammasome and inflammatory diseases by directly targeting NEK7

doi: 10.1016/j.xcrm.2023.101310

Figure Lengend Snippet:

Article Snippet: Entrectinib , TargetMol , Cat#T3678.

Techniques: Recombinant, LDH Cytotoxicity Assay, Enzyme-linked Immunosorbent Assay, Software

Journal: Molecular Cancer Therapeutics

Article Title: Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations

doi: 10.1158/1535-7163.MCT-25-0025

Figure Lengend Snippet: FEP calculations predict potency loss due to G-to-R mutation. Experimental (∆∆G biochem ) and predicted (∆∆G FEP ) changes in binding free energy for each ROS1 TKI shown as the mean ± SEM. ∆∆G FEP was obtained through simulations involving growing glycine to arginine (G → R) or truncating arginine to glycine (R → G), or the average of the two directions. A–F represent crizotinib, entrectinib, lorlatinib, taletrectinib, repotrectinib, and zidesamtinib, respectively. R 2 denotes correlation coefficient, and RMSD denotes the root-mean-squared deviation between predicted and experimental data.

Article Snippet: Compounds were purchased from commercial sources: crizotinib (Combi-Blocks, #QE-4059; MedChemExpress, #HY-50878; SelleckChem), entrectinib (Ark Pharm Inc., #AK547001; Advanced ChemBlocks, #K13380; SelleckChem), lorlatinib (Ark Pharm Inc., # AK175603 ; eNovation Chemicals, #Y0975931; SelleckChem), taletrectinib (MedChemExpress, #HY-131003), repotrectinib (Ark Pharm Inc., #AK689211; MedChemExpress, #HY-103022; SelleckChem, #S8583; DC Chemicals, #DC10463), and N -ethyl- N -nitrosourea (ENU; Sigma, #D2650).

Techniques: Mutagenesis, Binding Assay

Journal: Annals of Oncology

Article Title: Crizotinib resistance: implications for therapeutic strategies

doi: 10.1093/annonc/mdw305

Figure Lengend Snippet: Next-generation ALK inhibitors

Article Snippet: Entrectinib , Ignyta , Investigational , Phase 1/2a study of entrectinib in patients with advanced solid tumors harboring NTRK, ROS1, or ALK alterations [ {"type":"clinical-trial","attrs":{"text":"NCT02097810","term_id":"NCT02097810"}} NCT02097810 ] Phase 2 basket study of entrectinib in patients with solid tumors harboring NTRK, ROS1, or ALK rearrangements [ {"type":"clinical-trial","attrs":{"text":"NCT02568267","term_id":"NCT02568267"}} NCT02568267 ].

Techniques:

Journal: Molecules

Article Title: Approved Small-Molecule ATP-Competitive Kinases Drugs Containing Indole/Azaindole/Oxindole Scaffolds: R&D and Binding Patterns Profiling

doi: 10.3390/molecules28030943

Figure Lengend Snippet: Indole/azaindole/oxindole-containing ATP-competitive kinase inhibitors in clinical applications.

Article Snippet: 9l , Entrectinib , Genentech, South San Francisco, CA, USA , Solid tumors (e.g., breast cancer, cholangiocarcinoma, colorectal cancer, gynecological cancer, pancreatic cancer, and thyroid cancer) harboring NTRK1/2/3 or ROS1 gene fusions , Japan (2019) [ ] , adult and pediatric patients with NTRK fusion-positive, advanced or recurrent solid tumors.

Techniques: Functional Assay, Mutagenesis