PF-04979064

Names

[ CAS No. ]:
1220699-06-8

[ Name ]:
PF-04979064

[Synonym ]:
pf-04979064
pf04979064 /pf-04979064
1-{1-[(2S)-2-Hydroxypropanoyl]-4-piperidinyl}-3-methyl-8-(6-methyl-3-pyridinyl)-1,3-dihydro-2H-imidazo[4,5-c][1,5]naphthyridin-2-one
2H-Imidazo[4,5-c][1,5]naphthyridin-2-one, 1,3-dihydro-1-[1-[(2S)-2-hydroxy-1-oxopropyl]-4-piperidinyl]-3-methyl-8-(6-methyl-3-pyridinyl)-

Biological Activity

[Description]:

PF-04979064 is a potent and selective PI3K/mTOR dual kinase inhibitor with Kis of 0.13 nM and 1.42 nM for PI3Kα and mTOR, respectively.

[Related Catalog]:

Research Areas >> Cancer

[Target]

PI3Kα:0.13 nM (Ki)

PI3Kγ:0.111 nM (Ki)

PI3Kδ:0.122 nM (Ki)

mTOR:1.42 nM (Ki)

[In Vitro]

PF-04979064 is tested against human class I PI3K isoforms PI3Kα, PI3Kγ, and PI3Kδ, with PI3Kα Ki of 0.13 nM, PI3Kγ Ki of 0.111 nM, and PI3Kδ Ki of 0.122 nM[1].

[In Vivo]

PF-04979064 is progressed to rat in vivo PK studies and exhibits robust PK profile: Vdss=5.23 L/kg, Cl=19.3 mL/min/kg, T1/2=1.85 h, and F%=61%[1].

[References]

[1]. Cheng H et al. Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design. ACS Med Chem Lett, 2012 Nov 7, 4(1):91-7.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
682.0±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₄H₂₆N₆O₃

[ Molecular Weight ]:
446.502

[ Flash Point ]:
366.3±31.5 °C

[ Exact Mass ]:
446.206635

[ PSA ]:
106.14000

[ LogP ]:
0.35

[ Vapour Pressure ]:
0.0±2.2 mmHg at 25°C

[ Index of Refraction ]:
1.668

[ Storage condition ]:
2-8℃

Safety Information

[ Symbol ]:

GHS06

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301

[ Precautionary Statements ]:
P301 + P310

[ RIDADR ]:
UN 2811 6.1 / PGIII

Related Compounds

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