Journal: Scientific Reports

Article Title: Design, in silico studies and biological evaluation of novel chalcones tethered triazolo[3,4- a ]isoquinoline as EGFR inhibitors targeting resistance in non-small cell lung cancer

doi: 10.1038/s41598-024-76459-x

Figure Lengend Snippet: Inhibitory activities of chalcones 3e and 3f against EGFR-TKs compared to Lapatinib, Gefitinib, and Erlotinib as reference standards.

Article Snippet: The EGFR proteins (EGFR WT , EGFR T790M and EGFR L858R ) were obtained from Signalchem (BC V6V 2J2, Canada).

Techniques:

Journal: Scientific Reports

Article Title: Design, in silico studies and biological evaluation of novel chalcones tethered triazolo[3,4- a ]isoquinoline as EGFR inhibitors targeting resistance in non-small cell lung cancer

doi: 10.1038/s41598-024-76459-x

Figure Lengend Snippet: Selectivity index of the tested compounds 3e and 3f relative to the drugs for EGFR proteins: EGFR L858R , EGFR T790M , and EGFR wt . Selectively index (SI a ) = EGFR WT IC 50 / EGFR L858R IC 50 value, Selectively index (SI b ) = EGFR WT IC 50 / EGFR T790M IC 50 value.

Article Snippet: The EGFR proteins (EGFR WT , EGFR T790M and EGFR L858R ) were obtained from Signalchem (BC V6V 2J2, Canada).

Techniques:

Journal: Cancer Science

Article Title: LS‐106, a novel EGFR inhibitor targeting C797S, exhibits antitumor activities both in vitro and in vivo

doi: 10.1111/cas.15229

Figure Lengend Snippet: Structure and kinase inhibitory activity of LS‐106. A, Chemical structure of compound LS‐106. B, The kinase inhibitory activity of LS‐106 against EGFR 19del/T790M/C797S , EGFR L858R/T790M/C797S , EGFR 19del/T790M , EGFR L858R/T790M , EGFR 19del , and EGFR wt . Data are shown as mean ± SD. C, The docking structure of LS‐106 with EGFR L858R/T790M/C797S (protein from PDB ID: 6LUD). The EGFR kinase is shown in grey stick and ribbon representation. LS‐106 is shown in green and blue stick. Hydrogen bonds are indicated by yellow hatched lines to key amino acids

Article Snippet: EGFR 19del/T790M (#E10‐122KG) kinase protein was purchased from SignalChem.

Techniques: Activity Assay

Journal: Cancer Science

Article Title: LS‐106, a novel EGFR inhibitor targeting C797S, exhibits antitumor activities both in vitro and in vivo

doi: 10.1111/cas.15229

Figure Lengend Snippet: The kinase inhibitory activity of LS‐106 against different EGFR mutations (IC 50 s, nmol/L)

Article Snippet: EGFR 19del/T790M (#E10‐122KG) kinase protein was purchased from SignalChem.

Techniques: Activity Assay

Journal: Cancer Science

Article Title: LS‐106, a novel EGFR inhibitor targeting C797S, exhibits antitumor activities both in vitro and in vivo

doi: 10.1111/cas.15229

Figure Lengend Snippet: Inhibition activity of LS‐106 on BaF3 cells expressing different EGFR mutations. A, The proliferative inhibition of LS‐106 and osimertinib were measured in BaF3‐EGFR 19del/T790M/C797S cells, BaF3‐EGFR L858R/T790M/C797S cells, and BaF3‐EGFR 19del/T790M cells, respectively. B, The expression of phospho‐EGFR in BaF3‐EGFR 19del/T790M/C797S and BaF3‐EGFR L858R/T790M/C797S cells treated with LS‐106 or osimertinib were analyzed by Western blotting. The gray value was quantified by Image J software. Data are shown as mean ± SEM and were analyzed using t test, * P < .05, ** P < .01, *** P < .001

Article Snippet: EGFR 19del/T790M (#E10‐122KG) kinase protein was purchased from SignalChem.

Techniques: Inhibition, Activity Assay, Expressing, Western Blot, Software

Journal: Cancer Science

Article Title: LS‐106, a novel EGFR inhibitor targeting C797S, exhibits antitumor activities both in vitro and in vivo

doi: 10.1111/cas.15229

Figure Lengend Snippet: The apoptosis‐inducing effect of LS‐106 in EGFR–triple‐mutant cells. A, Cell apoptosis was measured in BaF3‐EGFR 19del/T790M/C797S cells after incubation with LS‐106 or osimertinib for 48 h. B, Cell apoptosis was measured in PC‐9‐OR cells after incubation with LS‐106 or osimertinib for 48 h. Apoptosis rates were analyzed based on the data of three independent tests. Data are shown as mean ± SD and were analyzed using t test, * P < .05, ** P < .01, *** P < .001

Article Snippet: EGFR 19del/T790M (#E10‐122KG) kinase protein was purchased from SignalChem.

Techniques: Mutagenesis, Incubation