Cat. No. 4823
Alternative Name: PKI-587
Chemical Name: N-[4-[[4-(Dimethylamino)-1-piperidi
Biological ActivityPotent and selective dual inhibitor of PI 3-kinase/mTOR (IC50 values are 0.4, 1.6 and 5.4 nM for PI 3-Kα, mTOR and PI 3-Kγ respectively). Exhibits selectivity over 234 other protein kinases (IC50 >10 μM). Potently inhibits tumor cell growth in 37 different tumor cell lines (IC50 < 100 nM). Also exhibits antitumor activity in MDA-361, HCT-116, H1975 and U87MG xenograft models.
Licensing InformationSold for research purposes under agreement from Pfizer Inc.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Safety Data Sheet
Mallon et al (2011) Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor. Clin.Cancer Res. 17 3193. PMID: 21325073.
Venkatesan et al (2010) Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor. J.Med.Chem. 53 2636. PMID: 20166697.
If you know of a relevant reference for this product please let us know.
Citations are publications that use Tocris products.
Do you know of a great paper that uses PF 05212384 from Tocris? If so please let us know.
View Related Products by Product Action
Keywords: PF 05212384, supplier, PF05212384, antitumor, antitumour, PI3-K, phosphoinositide, 3-kinases, mTOR, mammalian, target, of, rapamycin, inhibitors, inhibits, PKI587, Pfizer, Tocris Bioscience, PI 3-kinase Inhibitor products
Find multiple products by catalog number
New Products in this Area
Potent and selective PFKFB3 inhibitorSTOCK2S 26016
Lysine deficient protein kinase (WNK) signaling inhibitorrac-CCT 250863
Potent Nek2 inhibitorRoscovitine
Potent, selective cyclin-dependent kinase inhibitorEnzastaurin
Potent PKCβ inhibitorBMS 265246
Potent cdk1/2 inhibitorAutocamtide-2-related inhibitory peptide, myristoylated
CaM kinase II inhibitor; enhanced cell permeable derivative of Autocamtide-2-related inhibitory peptideMP A08
Selective ATP competitive SphK1 and 2 inhibitor; cell permeableAkti-1/2
Potent and selective dual Akt1 and 2 inhibitorVX 680
High affinity and selective Aurora kinase inhibitorImatinib mesylate
Potent and selective v-Abl tyrosine kinase inhibitor; also inhibits PDGFR and c-kitTGX 221
Potent and selective PI 3-kinase β inhibitorPF 543 hydrochloride
Potent and selective SphK1 inhibitorJX 06
Potent and selective pyruvate dehydrogenase kinase (PDK) 1/2/3 inhibitorMRT 68601 hydrochloride
Potent TBK1 inhibitor
Follow Tocris on LinkedIn
Visit our LinkedIn page for the latest Tocris news, events and updates.