Inhibition of GST-tagged SOS1 (564 to 1049 amino acids) (unknown origin) assessed as reduction SOS1/6xHis-Tev-tagged K-Ras G12D mutant (1 to 169 residues) interaction incubated for 30 mins by AlphaLISA method
Induction of apoptosis in human NCI-H358 cells grown under 3D anchorage-independent soft-agar conditions at grown under 3D anchorage-independent soft-agar conditions assessed as induction of PARP cleavage at 1 uM in presence of 125 nM of afatinib incubated for 24 hrs by mesoscale assay
Inhibition of SOS1 in human MIAPaCa2 cells grown under 3D anchorage-independent soft-agar conditions at assessed as ERK1/2 phosphorylation at Thr202/Tyr204 residues at 1 uM in presence of 50 nM trametinib incubated for 2 to 8 hrs by Western blotting analysis relative to control
Induction of apoptosis in human NCI-H358 cells grown under 3D anchorage-independent soft-agar conditions at grown under 3D anchorage-independent soft-agar conditions assessed as induction of PARP cleavage at 1 uM incubated for 24 to 72 hrs by mesoscale assay
Inhibition of SOS1 in human MIAPaCa2 cells grown under 3D anchorage-independent soft-agar conditions at assessed as suppression of increase in MEK1/2 phosphorylation at Ser 217/221 residues at 1 uM in presence of 25 to 50 nM trametinib incubated for 2 to 8 hrs by Western blotting analysis
Antitumor activity against human MIAPaCa2 cells grown under 3D anchorage-independent soft-agar conditions at xenografted in BomTacNMRI-Foxn1 nu mouse assessed as inhibition of tumor growth at 50 mg/kg, po BID relative to control
Antitumor activity against human MIAPaCa2 cells grown under 3D anchorage-independent soft-agar conditions at xenografted in BomTacNMRI-Foxn1 nu mouse assessed as inhibition of tumor regression at 50 mg/kg, po BID relative to control
Antitumor activity against human MIAPaCa2 cells grown under 3D anchorage-independent soft-agar conditions at xenografted in BomTacNMRI-Foxn1 nu mouse assessed as inhibition of tumor growth at 50 mg/kg, po BID co-treated with 0.05 mg/kg, po BID trametinib relative to control
Antitumor activity against human MIAPaCa2 cells grown under 3D anchorage-independent soft-agar conditions at xenografted in BomTacNMRI-Foxn1 nu mouse assessed as inhibition of tumor growth at 50 mg/kg, po BID co-treated with 0.125 mg/kg, po BID trametinib relative to control
Antitumor activity against human MIAPaCa2 cells grown under 3D anchorage-independent soft-agar conditions at xenografted in BomTacNMRI-Foxn1 nu mouse assessed as inhibition of tumor regression at 50 mg/kg, po BID co-treated with 0.125 mg/kg, po BID trametinib relative to control
Induction of apoptosis in human A549 cells grown under 3D anchorage-independent soft-agar conditions at grown under 3D anchorage-independent soft-agar conditions assessed as induction of PARP cleavage at 1 uM in presence of 10 nM of paclitaxel incubated for 24 to 48 hrs by mesoscale assay
Toxicity in BomTacNMRI-Foxn1 nu mouse xenografted with human MIAPaCa2 cells grown under 3D anchorage-independent soft-agar conditions at assessed as drug tolerability at 50 mg/kg, po BID co-treated with 10 mg/kg, iv paclitaxel dosed in q7d regime
Antitumor activity against human MIAPaCa2 cells grown under 3D anchorage-independent soft-agar conditions at xenografted in BomTacNMRI-Foxn1 nu mouse assessed as inhibition of tumor growth at 50 mg/kg, po BID co-treated with 10 mg/kg, iv paclitaxel dosed in q7d regime relative to control
Toxicity in BomTacNMRI-Foxn1 nu mouse xenografted with human MIAPaCa2 cells grown under 3D anchorage-independent soft-agar conditions at assessed as drug tolerability at 12 mg/kg, po BID co-treated with 50 mg/kg, ip gemcitabine dosed in q4d regime
Antitumor activity against human MIAPaCa2 cells grown under 3D anchorage-independent soft-agar conditions at xenografted in BomTacNMRI-Foxn1 nu mouse assessed as inhibition of tumor growth at 12 mg/kg, po BID co-treated with 50 mg/kg, ip gemcitabine dosed in q4d regime relative to control
Antitumor activity against human MIAPaCa2 cells grown under 3D anchorage-independent soft-agar conditions at xenografted in BomTacNMRI-Foxn1 nu mouse assessed as inhibition of tumor growth at 12 mg/kg, po BID relative to control
Growth inhibition of human PC9 cells grown under 3D anchorage-independent soft-agar conditions at 61.7 nM incubated for 14 days in presence of 1 nM Afatinib by alamar blue dye based assay relative to control
Growth inhibition of human PC9 cells grown under 3D anchorage-independent soft-agar conditions at 61.7 nM incubated for 14 days in presence of 0.333 nM Afatinib by alamar blue dye based assay relative to control
Growth inhibition of human PC9 cells grown under 3D anchorage-independent soft-agar conditions at 61.7 nM incubated for 14 days in presence of 0.111 nM Afatinib by alamar blue dye based assay relative to control
Growth inhibition of human PC9 cells grown under 3D anchorage-independent soft-agar conditions at 61.7 nM incubated for 14 days in presence of 0.037 nM Afatinib by alamar blue dye based assay relative to control