Potency data for probe ACBI3 and control cis-ACBI3
In vitro potency
| Target name | Target information | Species | Assay description | ACBI3 | cis-ACBI3 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| KRAS (G12D) | human recombinant N-terminally His 6 -tagged KRAS G12D | Homo sapiens | SPR (KRAS G12D): GDP was added. | KD = 5 nM ± 1.000 nM (n=3) | PMID: 39298590 | |
| KRAS (G12V) | human recombinant N-terminally His 6 -tagged KRAS G12V | Homo sapiens | SPR (KRAS G12V): GDP was added. | KD = 4 nM ± 1.000 nM (n=3) | PMID: 39298590 | |
| KRAS (G12D) | human recombinant N-terminally His 6 -tagged KRAS G12D | Homo sapiens | Fluorescence Polarization (KRAS G12D): VCB complex consisting of VHL (54-213), Elongin C (17-112) and Elongin B was added | KD = 4 nM ± 1.000 nM (n=3) | PMID: 39298590 |
In cell potency
| Target name | Target information | Species | Assay description | ACBI3 | cis-ACBI3 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| KRAS (G12D) | GP5d cells | Homo sapiens | Cellular KRAS G12D degradation: Assay: capillary electrophoresis using the antibody KRASG12D normalized by GAPDH, 24 h | DC50 = 2 nM | DC50 = 1 µM | PMID: 39298590 |
| KRAS (G12V) | SW620 cells | Homo sapiens | Cellular KRAS G12V degradation: Assay: capillary electrophoresis using the antibody KRASG12V normalized by GAPDH, 24 h | DC50 = 7 nM | PMID: 39298590 | |
| KRAS | GP5d cells | Homo sapiens | Cellular proliferation (GP5d cells): CellTiterGlo assay, 5 days | IC50 = 5 nM | IC50 = 1 µM | PMID: 39298590 |
| KRAS | SW620 cells | Homo sapiens | Cellular proliferation (SW620 cells): CellTiterGlo assay, 5 days | IC50 = 15 nM | PMID: 39298590 |