Table 4.

Antitumor activity of wortmannin analogues against human tumor xenografts in scid mice

Tumor (Doubling Time)Initial Tumor Volume (mm3)Compoundmg/kg/dRouteScheduleT/C% (d)Growth Delay (d)Log10 Cell KillP
OvCar-3 ovarian (6.0 d)120Wortmannin0.75i.p.Q1D × 947 (40)50.5*
120PX-8668i.p.Q1D × 930 (40)121.2*
120PX-86713i.p.Q1D × 941 (40)60.6*
120PX-88112i.p.Q1D × 952 (40)80.8*
HT-29 colon (5.2 d)180Wortmannin0.75i.p.Q1D × 936 (16)50.3*
170PX-86612i.p.Q1D × 939 (16)60.4*
170PX-86713i.p.Q1D × 980 (16)00
170PX-88112i.p.Q1D × 962 (16)20.2
A-549 lung (5.8 d)65PX-8666i.p.Q1D × 962 (32)40.2
65PX-8669i.p.Q1D × 926 (32)80.4*
60PX-86612i.v.Q2D × 545 (21)50.7*
60PX-8664p.o.Q2D × 547 (21)60.9*
  • NOTE: Mice were implanted s.c. with 107 tumor cells. When the tumor volume reached the value shown, the mice were randomized into groups of eight and drug treatment started at the indicated doses. The doubling time for each tumor during its log phase of growth is shown in parentheses.

  • * P < 0.05 compared with non-drug-treated control tumor growth rate.