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Year Number of Results
2010 2
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2013 1
2014 6
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60 results
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PKI-587 enhances radiosensitization of hepatocellular carcinoma by inhibiting the PI3K/AKT/mTOR pathways and DNA damage repair.
Xie Y, Liu C, Zhang Y, Li A, Sun C, Li R, Xing Y, Shi M, Wang Q. Xie Y, et al. PLoS One. 2021 Oct 19;16(10):e0258817. doi: 10.1371/journal.pone.0258817. eCollection 2021. PLoS One. 2021. PMID: 34665844 Free PMC article.
In vivo, the combination of radiation with PKI-587 significantly inhibited tumor growth. These findings suggest the usefulness of PKI-587 on radiosensitization of HCC cells by inhibiting the PI3K/AKT/mTOR and DNA damage repair pathways. The combination …
In vivo, the combination of radiation with PKI-587 significantly inhibited tumor growth. These findings suggest the usefulness …
PKI-587 enhances chemosensitivity of oxaliplatin in hepatocellular carcinoma through suppressing DNA damage repair pathway (NHEJ and HR) and PI3K/AKT/mTOR pathway.
Zhang Y, Xie C, Li A, Liu X, Xing Y, Shen J, Huo Z, Zhou S, Liu X, Xie Y, Cao W, Ma Y, Xu R, Cai S, Tang X, Ma D. Zhang Y, et al. Am J Transl Res. 2019 Aug 15;11(8):5134-5149. eCollection 2019. Am J Transl Res. 2019. PMID: 31497229 Free PMC article.
In this research, we evaluated the effect of the dual PI3K/mTOR inhibitor, PKI-587, on the sensitivity of oxaliplatin in HCC. Two HCC cell lines (HepG2 and SK-Hep1) were used to analyze PKI-587 for DNA damage response, cell proliferation, clonogenic su …
In this research, we evaluated the effect of the dual PI3K/mTOR inhibitor, PKI-587, on the sensitivity of oxaliplatin in HCC. …
PKI-587 and sorafenib targeting PI3K/AKT/mTOR and Ras/Raf/MAPK pathways synergistically inhibit HCC cell proliferation.
Gedaly R, Angulo P, Hundley J, Daily MF, Chen C, Evers BM. Gedaly R, et al. J Surg Res. 2012 Aug;176(2):542-8. doi: 10.1016/j.jss.2011.10.045. Epub 2011 Nov 21. J Surg Res. 2012. PMID: 22261591
Phosphorylation of the key enzymes in the Ras/Raf/MAPK and PI3K/AKT/mTOR pathways was detected by Western blot. RESULTS: We found that PKI-587 is a more potent PI3K/mTOR inhibitor than PI-103. Combination of PKI-587 and sorafenib was a more effective i …
Phosphorylation of the key enzymes in the Ras/Raf/MAPK and PI3K/AKT/mTOR pathways was detected by Western blot. RESULTS: We found that PK
PKI-587 and sorafenib alone and in combination on inhibition of liver cancer stem cell proliferation.
Gedaly R, Galuppo R, Musgrave Y, Angulo P, Hundley J, Shah M, Daily MF, Chen C, Cohen DA, Spear BT, Evers BM. Gedaly R, et al. J Surg Res. 2013 Nov;185(1):225-30. doi: 10.1016/j.jss.2013.05.016. Epub 2013 May 25. J Surg Res. 2013. PMID: 23769634 Free PMC article.

PLC cells were more sensitive to PKI-587 than LCSC or Huh7 (P < 0.001). Interestingly, HuH7 cells were more sensitive to sorafenib than LCSC or PLC cells. Additionally, combination therapy with PKI-587 and sorafenib caused significantly more inhibit

PLC cells were more sensitive to PKI-587 than LCSC or Huh7 (P < 0.001). Interestingly, HuH7 cells were more sensitive to so

Oxaliplatin and Gedatolisib (PKI-587) Co-Loaded Hollow Polydopamine Nano-Shells with Simultaneous Upstream and Downstream Action to Re-Sensitize Drugs-Resistant Hepatocellular Carcinoma to Chemotherapy.
Zhang YC, Wu CG, Li AM, Liang Y, Ma D, Tang XL. Zhang YC, et al. J Biomed Nanotechnol. 2021 Jan 1;17(1):18-36. doi: 10.1166/jbn.2021.3014. J Biomed Nanotechnol. 2021. PMID: 33653494
Herein, we developed a hollow polydopamine nanoparticle (H-PDA)-based nano-delivery system (O/P-HP) that contained OXA and a dual PI3K/mTOR inhibitor PKI-587 with complementary effects for combating drug resistance in cancer chemotherapy. ...These values were signif …
Herein, we developed a hollow polydopamine nanoparticle (H-PDA)-based nano-delivery system (O/P-HP) that contained OXA and a dual PI3K/mTOR …
Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor.
Mallon R, Feldberg LR, Lucas J, Chaudhary I, Dehnhardt C, Santos ED, Chen Z, dos Santos O, Ayral-Kaloustian S, Venkatesan A, Hollander I. Mallon R, et al. Clin Cancer Res. 2011 May 15;17(10):3193-203. doi: 10.1158/1078-0432.CCR-10-1694. Epub 2011 Feb 15. Clin Cancer Res. 2011. PMID: 21325073
PKI-587 inhibited growth of 50 diverse human tumor cell lines at IC(50) values of less than 100 nmol/L. ...PKI-587 at 25 mg/kg (once weekly) shrank large (1,000 mm(3)) MDA-MB-361 tumors and suppressed tumor regrowth. ...
PKI-587 inhibited growth of 50 diverse human tumor cell lines at IC(50) values of less than 100 nmol/L. ...PKI-587
Inhibition of mTOR's Catalytic Site by PKI-587 Is a Promising Therapeutic Option for Gastroenteropancreatic Neuroendocrine Tumor Disease.
Freitag H, Christen F, Lewens F, Grass I, Briest F, Iwaszkiewicz S, Siegmund B, Grabowski P. Freitag H, et al. Neuroendocrinology. 2017;105(1):90-104. doi: 10.1159/000448843. Epub 2016 Aug 12. Neuroendocrinology. 2017. PMID: 27513674 Free PMC article.
AIM: We assessed the effects of PKI-587 in different GEP-NEN tumor models, including the poorly differentiated cell line LCC-18, and compared them with those of the established mTORC1 inhibitor everolimus. METHODS: We treated BON, QGP-1, KRJ-I, and LCC-18 cell lines …
AIM: We assessed the effects of PKI-587 in different GEP-NEN tumor models, including the poorly differentiated cell line LCC-1 …
The dual specificity PI3K/mTOR inhibitor PKI-587 displays efficacy against T-cell acute lymphoblastic leukemia (T-ALL).
Gazi M, Moharram SA, Marhäll A, Kazi JU. Gazi M, et al. Cancer Lett. 2017 Apr 28;392:9-16. doi: 10.1016/j.canlet.2017.01.035. Epub 2017 Feb 1. Cancer Lett. 2017. PMID: 28159681 Free article.
Furthermore, we observed that PKI-587 blocked proliferation and colony formation of T-ALL cell lines. Additionally, PKI-587 selectively abrogated PI3K/mTOR signaling without affecting MAPK signaling both in in vitro and in vivo. ...
Furthermore, we observed that PKI-587 blocked proliferation and colony formation of T-ALL cell lines. Additionally, PKI
Dual PI3K/mTOR inhibitors, GSK2126458 and PKI-587, suppress tumor progression and increase radiosensitivity in nasopharyngeal carcinoma.
Liu T, Sun Q, Li Q, Yang H, Zhang Y, Wang R, Lin X, Xiao D, Yuan Y, Chen L, Wang W. Liu T, et al. Mol Cancer Ther. 2015 Feb;14(2):429-39. doi: 10.1158/1535-7163.MCT-14-0548. Epub 2014 Dec 12. Mol Cancer Ther. 2015. PMID: 25504751
In the present study, we evaluated whether inhibition of PI3K/mTOR by two novel dual inhibitors, GSK2126458 and PKI-587, could suppress tumor progression and sensitize NPC cells to radiation. ...The combination of IR with a dual PI3K/mTOR inhibitor, GSK2126458 or …
In the present study, we evaluated whether inhibition of PI3K/mTOR by two novel dual inhibitors, GSK2126458 and PKI-587, could …
The dual PI3K/mTOR inhibitor PKI-587 enhances sensitivity to cetuximab in EGFR-resistant human head and neck cancer models.
D'Amato V, Rosa R, D'Amato C, Formisano L, Marciano R, Nappi L, Raimondo L, Di Mauro C, Servetto A, Fusciello C, Veneziani BM, De Placido S, Bianco R. D'Amato V, et al. Br J Cancer. 2014 Jun 10;110(12):2887-95. doi: 10.1038/bjc.2014.241. Epub 2014 May 13. Br J Cancer. 2014. PMID: 24823695 Free PMC article.
METHODS: Different human squamous cancer cell lines sensitive or resistant to cetuximab were tested for the dual PI3K/mTOR inhibitor PF-05212384 (PKI-587), alone and in combination, both in vitro and in vivo. RESULTS: Treatment with PKI-587 enhances se …
METHODS: Different human squamous cancer cell lines sensitive or resistant to cetuximab were tested for the dual PI3K/mTOR inhibitor PF-0521 …
60 results