Unknown

Dataset Information

0

Initial testing (stage 1) of LCL161, a SMAC mimetic, by the Pediatric Preclinical Testing Program.


ABSTRACT: LCL161, a SMAC mimetic, was tested against the PPTP in vitro panel (1.0?nM to 10.0?µM) and the PPTP in vivo panels (30 or 75?mg/kg [solid tumors] or 100?mg/kg [ALL]) administered orally twice in a week. LCL161 showed a median relative IC(50) value of >10?µM, being more potent against several leukemia and lymphoma lines. In vivo LCL161 induced significant differences in EFS distribution in approximately one-third of solid tumor xenografts (osteosarcoma and glioblastoma), but not in ALL xenografts. No objective tumor responses were observed. In vivo LCL161 demonstrated limited single agent activity against the pediatric preclinical models studied.

SUBMITTER: Houghton PJ 

PROVIDER: S-EPMC3253328 | biostudies-literature | 2012 Apr

REPOSITORIES: biostudies-literature

altmetric image

Publications

Initial testing (stage 1) of LCL161, a SMAC mimetic, by the Pediatric Preclinical Testing Program.

Houghton Peter J PJ   Kang Min H MH   Reynolds C Patrick CP   Morton Christopher L CL   Kolb E Anders EA   Gorlick Richard R   Keir Stephen T ST   Carol Hernan H   Lock Richard R   Maris John M JM   Billups Catherine A CA   Smith Malcolm A MA  

Pediatric blood & cancer 20110616 4


LCL161, a SMAC mimetic, was tested against the PPTP in vitro panel (1.0 nM to 10.0 µM) and the PPTP in vivo panels (30 or 75 mg/kg [solid tumors] or 100 mg/kg [ALL]) administered orally twice in a week. LCL161 showed a median relative IC(50) value of >10 µM, being more potent against several leukemia and lymphoma lines. In vivo LCL161 induced significant differences in EFS distribution in approximately one-third of solid tumor xenografts (osteosarcoma and glioblastoma), but not in ALL xenografts  ...[more]

Similar Datasets

| S-EPMC2731000 | biostudies-literature
| S-EPMC4244112 | biostudies-literature
| S-EPMC2752378 | biostudies-literature
| S-EPMC2794954 | biostudies-literature
| S-EPMC5587189 | biostudies-literature
| S-EPMC3004092 | biostudies-literature
| S-EPMC2965797 | biostudies-literature
| S-EPMC3115432 | biostudies-literature
| S-EPMC3154460 | biostudies-literature
| S-EPMC4225043 | biostudies-literature