Table 2.

Cross-resistance profile to standard-of-care chemotherapeutics and other unconjugated drugs

361: Parental versus TM-resistantJIMT1: Parental versus TM-resistant
Drug classTreatmentParental (IC50, nmol/L)TM (IC50, nmol/L)Relative resistanceParental (IC50, nmol/L)TM (IC50, nmol/L)Relative resistance
Tubulin: depolymerizingDM1-SMe11423.8×16553.4×
Vinblastine2.82.91.0×1.53.52.3×
MMAD0.100.101.0×0.060.335.5×
Aur-82540.440.421.0×0.281.45.0×
Tubulin: polymerizingPaclitaxel5.77.81.4×7.5141.9×
Docetaxel3.85.21.4×2.93.81.3×
DNA: topoisomerase inhibitorsDoxorubicin1704102.4×1603502.2×
Etoposide11,00025,0002.3×4,70013,0002.8×
Camptothecin3602900.8×691602.3×
DNA: anti-metabolites5-Fluorouracil7,50023,0003.1×45,00036,0000.8×
Gemcitabine25271.1×22180.8×
DNA: alkylatingOxaliplatin13,0004,0000.3×30,00021,0000.7×
Signaling inhibitorsHer2 kinase inhibitor2,2004700.2×1,0001,3001.3×
Rapamycin analogue5,6003,1000.6×24,00023,0001.0×

NOTE: Parental and TM-resistant cell lines were treated with the indicated chemotherapeutic agent and cytotoxicity assessed as indicated in Materials and Methods. Data are mean IC50 from 2–6 determinations for each compound, rounded to 2 significant figures. Aur-8254 is an auristatin analogue. Her2 kinase inhibitor is neratinib; rapamycin analogue is temsirolimus. Relative resistance is the ratio of the mean IC50 for the TM-resistant cell line versus the corresponding parental cell line.