Table 2.

In vivo activity of PHA-848125 in human xenograft tumor models

ModelDose/schedule (mg/kg twice a day/D1–D10)Maximal % TGI (day)Maximal weight loss (%)
A2780 ovarian cancer (nude mice)4091% (11)10
HL60 AML (SCID mice)4084% (11)9
HCT116 colon cancer (nude mice)4064% (11)15
BX-PC3 pancreatic cancer (nude mice)4074% (10)10
CAPAN-1 pancreatic cancer (nude mice)4065% (11)11
DU-145 prostatic cancer (nude mice)4091% (11)0
A375 melanoma (nude mice)4069% (11)9
A549 non–small cell lung cancer (nude mice)4073% (11)0
MiaPaca-2 pancreatic adenocarcinoma (nude mice)4070% (11)0

NOTE: The compound was administered twice a day at 40 mg/kg for 10 consecutive days (D1–D10). Percentage of inhibition compared with the vehicle-treated group and the maximal weight loss were calculated 1 d after the stop of treatment.