Table 1.

The antiproliferative activity of RAD001 is associated with G1 accumulation

RAD001 sensitivityCell lineTissue of originMean RAD001 IC50 (±SD), nmol/Lp53 statusTreatment 24 h (20 nmol/L RAD001)% Cells in G1 (cell cycle)
SensitiveBT474Breast0.55 ± 0.12MutantDMSO76
RAD00194
SensitiveMCF7Breast0.60 ± 0.10Wild typeDMSO55
RAD00172
SensitiveSKBR3Breast0.74 ± 0.34MutantDMSO63
RAD00183
SensitiveLN401Glioblastoma1.5 ± 0.30N.d.DMSO68
RAD00178
SensitiveT47DBreast1.8 (1.1; 2.5)MutantDMSO65
RAD00170
SensitiveA549Lung2.4 (1.2; 3.7)Wild typeDMSO54
RAD00169
SensitiveMDA-MB-231Breast7.2 ± 4.1MutantDMSO54
RAD00161
SensitiveDU145Prostate10.3 ± 2.2MutantDMSO56
RAD00162
SensitiveHCT15Colon65 ± 23MutantDMSO42
RAD00151
InsensitivePC3MProstate149 ± 46MutantDMSO57
RAD00158
InsensitiveLN428Glioblastoma327 ± 206N.d.DMSO72
RAD00173
InsensitiveKB31Epidermoid1778 ± 800N.d.DMSO54
RAD00155
InsensitiveHCT116Colon4125 ± 1853Wild typeDMSO55
RAD00155

NOTE: The antiproliferative activity of RAD001 was measured by the methylene blue assay, defining IC50 values for RAD001 treatment in a mixed panel of human cancer cell lines (left). After 24 h treatment with optimal (20 nmol/L) RAD001, cells were subjected to cell cycle analysis by flow cytometry. A G1 accumulation was observed in RAD001-sensitive cells only (IC50 ≤ 100 nmol/L; right). There was no evidence of a sub-G1 population (not shown). Cells with known p53 status are noted.

Abbreviation: N.d., not defined.