Abstract

The antiproliferative effects of 111In-DTPA-hEGF on breast cancer cells expressing high levels of EGFR were compared with those of chemotherapeutic agents or γ-radiation. MDA-MB-468 cells were cultured with 111In-DTPA-hEGF (30 MBq/μg, 1.8 × 10 5 MBq/μmol), DTPA-hEGF, methotrexate, doxorubicin, paclitaxel or 5-fluorouracil. Cell growth was measured colorimetrically. The IC 50 for 111In-DTPA-hEGF was <70 pM (11 kBq/mL) versus 500 pM for DTPA-hEGF. The IC 50 for paclitaxel, methotrexate, doxorubicin and 5-fluorouracil was 6 nM, 15 nM, 20 nM and 4 μM respectively. 111In-DTPA-hEGF (70 pM, 11 kBq/mL) delivered approx. 6 Gy to breast cancer cells producing growth inhibition equivalent to 4 Gy of γ-radiation. We conclude that 111In-DTPA-hEGF exhibited potent antiproliferative effects towards breast cancer cells at concentrations much lower than chemotherapeutic agents and equivalent to those produced by several Gy of high dose rate γ-radiation.

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