TABLE 3.
Cytotoxicity of ceralasertib in parental and ABCB1 or ABCG2 knockout cells with or without BCRP inhibition.
| Cell line | IC50 ± SD (μM) | Resistance fold |
|---|---|---|
| SW620-ABCB1ko | 0.39 ± 0.18 | 1 |
| SW620/Ad300-ABCB1ko | 1.95 ± 0.55 | 5.00 |
| SW620-ABCB1ko + Verapamil | 0.36 ± 0.21 | 0.92 |
| SW620/Ad300-ABCB1ko + Verapamil | 1.26 ± 0.16 | 3.23 |
| NCI-H460-ABCG2ko | 1.04 ± 0.09 | 1.00 |
| NCI-H460/TPT10-ABCG2ko | 1.24 ± 0.06 | 1.19 |
| NCI-H460-ABCG2ko + Ko143 | 0.91 ± 0.14 | 0.86 |
| NCI-H460/TPT10-ABCG2ko + Ko143 | 0.94 ± 0.12 | 0.90 |
Verapamil is a selective inhibitor of P-gp transporter and ko143 is a selective inhibitor of BCRP transporter. IC50 values are represented as mean ± SD of at least three independent experiments performed in triplicate. Resistance fold was calculated by dividing the IC50 values of substrates in the presence or absence of inhibitor by the IC50 of parental cells without inhibitor.