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Association details:
Evidence:
Evidence Level:
Sensitive: D – Preclinical
New
Title:

Antitumor Efficacy of PKI-587, a Highly Potent Dual PI3K/mTOR Kinase Inhibitor

Excerpt:
Exposure (24 hours) of H1975 to combined PKI-587 and HKI-272 (250 nmol/L) markedly increased suppression of p-Akt (T308; IC50 < 30 nmol/L), increased caspase 3/7 activity (Supplementary Fig. 5C), and induced cPARP at 30 nmol/L or more...When PKI-587 (5 mg/kg, d×5 once) was given in combination with HKI-272 (40 mg/kg, po daily) significantly (P < 0.02), more antitumor effect than either compound given alone was observed in a 14-day study...
DOI:
10.1158/1078-0432.CCR-10-1694