Potency data for probe Borussertib and control RL2578
In vitro potency
| Target name | Target information | Species | Assay description | Borussertib | RL2578 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| AKT1 | Homo sapiens | Homogeneous Time Resolved Fluorescence (HTRF) assay (AKT1) | IC50 = 0.8 nM ± 0.300 nM | IC50 = 9.2 µM | ||
| AKT2 | Homo sapiens | Homogeneous Time Resolved Fluorescence (HTRF) assay (AKT2) | IC50 = 59 nM ± 16.000 nM | |||
| AKT3 | Homo sapiens | Homogeneous Time Resolved Fluorescence (HTRF) assay (AKT3) | IC50 = 650 nM ± 170.000 nM |
In cell potency
| Target name | Target information | Species | Assay description | Borussertib | RL2578 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| AKT1 | Homo sapiens | NanoBRET assay (AKT1): SGC Frankfurt | EC50 = 26 nM ± 3.800 nM (n=3) | EC50 = 3.5 µM ± 1.500 µM (n=3) | ||
| AKT2 | Homo sapiens | NanoBRET assay (AKT2): SGC Frankfurt | EC50 = 250 nM ± 170.000 nM (n=3) | EC50 = 4.8 µM ± 0.900 µM (n=3) | ||
| AKT3 | Homo sapiens | NanoBRET assay (AKT3): SGC Frankfurt | EC50 = 29 nM ± 11.000 nM (n=3) | EC50 = 9.3 µM ± 0.660 µM (n=3) | ||
| ZR-75-1 cells (breast) | Homo sapiens | CellTiter-Glo luminescent cell viability assay (CTG) with ZR-75-1 cells | EC50 = 5 nM ± 1.000 nM | EC50 = 4.2 µM | PMID: 30996949 | |
| T-47D cells (breast) | Homo sapiens | CellTiter-Glo luminescent cell viability assay (CTG) with T-47D cells | EC50 = 50 nM ± 15.000 nM | PMID: 30996949 | ||
| AN3-CA cells (endometrium) | Homo sapiens | CellTiter-Glo luminescent cell viability assay (CTG) with AN3-CA cells | EC50 = 190 nM ± 90.000 nM | EC50 = 18 µM | PMID: 30996949 | |
| BT-474 cells (breast) | Homo sapiens | CellTiter-Glo luminescent cell viability assay (CTG) with BT-474 cells | EC50 = 370 nM ± 50.000 nM | PMID: 30996949 | ||
| MCF-7 cells (breast) | Homo sapiens | CellTiter-Glo luminescent cell viability assay (CTG) with MCF-7 cells | EC50 = 280 nM ± 90.000 nM | PMID: 30996949 |