PKI-587 is a highly potent dual PI3K/mTOR kinase inhibitor with IC50 of 0.4 nM and <0.1 ¦ÌM for PI3K-¦Á and mTOR, respectively. Intravenous administration of PKI-587 exhibits excellent antitumor activity in vitro and in vivo in both subcutaneous and orthotopic xenograft tumor models. Phosphorylation of PI3K/mTOR effectors (e.g., Akt) effectively inhibited by PKI-587. And PKI-587 induced apoptosis in human tumor cell lines with elevated PI3K/mTOR signaling. In vivo, PKI-587suppressed tumor growth in breast (MDA-MB-361, BT474), colon (HCT116), lung (H1975), and glioma (U87MG) xenograft models. PKI-587 (25 mg/kg, single dose i.v.) suppressed Akt phosphorylation [at threonine(T)308 and serine(S)473] for up to 36 hours, with cleaved PARP (cPARP) evident up to 18 hours in MDA-MB-361 tumors. PKI-587 also caused regression in other tumor models, and efficacy was enhanced when given in combination with PD0325901 (MEK 1/2 inhibitor), irinotecan (topoisomerase I inhibitor), or HKI-272 (neratinib, HER2 inhibitor).

June 21, 2017

prudect name : PKI-587 is a highly potent dual PI3K/mTOR kinase inhibitor with IC50 of 0.4 nM and <0.1 ¦ÌM for PI3K-¦Á and mTOR, respectively. Intravenous administration of PKI-587 exhibits excellent antitumor activity in vitro and in vivo in both subcutaneous and orthotopic xenograft tumor models. Phosphorylation of PI3K/mTOR effectors (e.g., Akt) effectively inhibited by PKI-587. And PKI-587 induced apoptosis in human tumor cell lines with elevated PI3K/mTOR signaling. In vivo, PKI-587suppressed tumor growth in breast (MDA-MB-361, BT474), colon (HCT116), lung (H1975), and glioma (U87MG) xenograft models. PKI-587 (25 mg/kg, single dose i.v.) suppressed Akt phosphorylation [at threonine(T)308 and serine(S)473] for up to 36 hours, with cleaved PARP (cPARP) evident up to 18 hours in MDA-MB-361 tumors. PKI-587 also caused regression in other tumor models, and efficacy was enhanced when given in combination with PD0325901 (MEK 1/2 inhibitor), irinotecan (topoisomerase I inhibitor), or HKI-272 (neratinib, HER2 inhibitor).
PKI-587

Synonyms: PF-05212384CAS NO: 1197160-78-3Molecular Formula: C32H41N9O4Molecular Weight: 615.73Purity: 99% minSolubility: In DMSOStorage: −20°C


web site: www.medchemexpress.com