Basic information Safety Supplier Related

PF-04979064

Basic information Safety Supplier Related

PF-04979064 Basic information

Product Name:
PF-04979064
Synonyms:
  • PF-04979064
  • (S)-1-(1-(2-hydroxypropanoyl)piperidin-4-yl)-3-methyl-8-(6-methylpyridin-3-yl)-1H-imidazo[4,5-c][1,5]naphthyridin-2(3H)-one
  • CS-2664
  • PF-04979064 ≥95%
  • PF 04979064;PF04979064
  • 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)-
  • PF-04979064 >=98% (HPLC)
  • 1,3-Dihydro-1-[1-[(2S)-2-hydroxy-1-oxopropyl]-4-piperidinyl]-3-methyl-8-(6-methyl-3-pyridinyl)-2H-imidazo[4,5-c][1,5]naphthyridin-2-one
CAS:
1220699-06-8
MF:
C24H26N6O3
MW:
446.5
Mol File:
1220699-06-8.mol
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PF-04979064 Chemical Properties

Boiling point:
682.0±55.0 °C(Predicted)
Density 
1.355±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO : 11 mg/mL (24.64 mM)
form 
Solid
pka
13.95±0.20(Predicted)
color 
White to yellow
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PF-04979064 Usage And Synthesis

Uses

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.

Biological Activity

PF-04979064 is an orally available, potent and selective PI3K/mTOR dual kinase inhibitor th at potently inhibits tumor growth in mouse xenografts.

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].

IC 50

PI3Kα: 0.13 nM (Ki); PI3Kγ: 0.111 nM (Ki); PI3Kδ: 0.122 nM (Ki); mTOR: 1.42 nM (Ki)

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. DOI:10.1021/ml300309h

PF-04979064Supplier

WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.
Tel
17702719238 18971495150;
Email
sales@sun-shinechem.com
Sichuan Wei Keqi Biological Technology Co., Ltd.
Tel
028-81700200 18116577057
Email
3003855609@qq.com
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Pharmacodia (Beijing) Co.,Ltd
Tel
+86-400-851-9921
Email
sales@pharmacodia.com
Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Email
info@efebio.com
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PF-04979064(1220699-06-8)Related Product Information