Table 1.

Activity of TMZ, DP68, and DP86 in glioma cultures

IC50 (μmol/L)
Cell lineMGMTEGFR amplifiedP53PTEN activityTMZDP86DP68TMZ/DP68
Established glioma cell line CyQuant assay
 T98G+++Mutant340 ± 21110 ± 911.3 ± 2.230
 U118MG+Mutant135 ± 4142 ± 710 ± 3.014
 U251Mutant60 ± 2168 ± 75.2 ± 0.612
 U251TMZND306 ± 2170 ± 133.6 ± 0.585
 U87MGWT43 ± 2367 ± 2014 ± 53
Established glioma line neurosphere assay
 U118NS+Mutant71 ± 1142 ± 92.7 ± 0.226
 U87NSWT7.5 ± 1.061 ± 25.9 ± 0.51.3
 U87NSTMZNDND153 ± 833 ± 34.1 ± 0.237
Patient-derived xenograft neurosphere assay
 GBM6+++EGFRvIIIMutantWT187 ± 3843 ± 241.3 ± 0.6144
 GBM12MutantMutantWT3.2 ± 0.319 ± 30.8 ± 0.14
 GBM12TMZ+++NDNDND500 ± 13225 ± 21.4 ± 0.1357

Abbreviations: ND, not determined; WT, wild-type.