PF-04979064

Modify Date: 2024-01-16 17:45:52

PF-04979064 Structure
PF-04979064 structure
Common Name PF-04979064
CAS Number 1220699-06-8 Molecular Weight 446.502
Density 1.4±0.1 g/cm3 Boiling Point 682.0±55.0 °C at 760 mmHg
Molecular Formula C24H26N6O3 Melting Point N/A
MSDS Chinese USA Flash Point 366.3±31.5 °C
Symbol GHS06
GHS06
Signal Word Danger

 Use of PF-04979064


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.

 Names

Name 1-(1-[(2S)-2-hydroxypropanoyl]piperidin-4-yl)-3-methyl-8-(6-methylpyridin-3-yl)-1,3-dihydro-2H-imidazo[4,5-c][1,5]naphthyridin-2-one
Synonym More Synonyms

 PF-04979064 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
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.

 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
GHS06
Signal Word Danger
Hazard Statements H301
Precautionary Statements P301 + P310
RIDADR UN 2811 6.1 / PGIII

 Synonyms

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)-
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Price: $106/10mM*1mLinDMSO

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