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PF-05212384 (PKI-587)PI3Kα, PI3Kγ and mTOR inhibitor

PF-05212384 (PKI-587)

Catalog No. B2179
Size Price Stock Qty
5mg $50.00 In stock
25mg $200.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

PF-05212384 (PKI-587)

Biological Activity

Description PF-05212384 (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ and mTOR with IC50 values of 0.4 nM, 5.4 nM and 1.6 nM, respectively.
Targets PI3Kα mTOR PI3Kγ      
IC50 0.4 nM 1.6 nM 5.4 nM      

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Chemical Properties

Cas No. 1197160-78-3 SDF Download SDF
Chemical Name 1-[4-[4-(dimethylamino)piperidine-1-carbonyl]phenyl]-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea
Canonical SMILES CN(C)C1CCN(CC1)C(=O)C2=CC=C(C=C2)NC(=O)NC3=CC=C(C=C3)C4=NC(=NC(=N4)N5CCOCC5)N6CCOCC6
Formula C32H41N9O4 M.Wt 615.73
Solubility Limited solubility Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

PF-05212384 is an inhibitor of PI3K/mTOR with IC50 values of 0.4nM, 6nM, 8nM, 6nM and 1.4nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and mTOR, respectively [1].

PF-05212384 is a pan-PI3K/mTORinhibitor and shows to be highly selective for PI3K and mTOR. Besides the wt P13K, PF-05212384 can also inhibit mutant P13K with IC50 values of 0.6nM for both H1047R and E545K mutants. In cellular assay, PF-05212384 potently inhibits tumor growth in MDA-361 and PC3-MM2 cell lines with IC50 values of 4nM and 13.1nM, respectively. Meanwhile, PF-05212384 suppresses the phosphorylation of PI3K/mTOR signaling pathway proteins in cells. It inhibits the phosphorylation of Akt as well as the Akt effector proteins including GSK3 kinase, ENOS and PRAS 40. Moreover, PF-05212384 has potent anti-tumor activity in a variety of xenograft models including H1975, BT474, HCT116, H1975 and U87MG [1, 2]

References:
[1] Venkatesan A M, Dehnhardt C M, Delos Santos E, et al. 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. Journal of medicinal chemistry, 2010, 53(6): 2636-2645.
[2] Mallon R, Feldberg L R, Lucas J, et al. Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor. Clinical Cancer Research, 2011, 17(10): 3193-3203.