ChemicalBook > CAS DataBase List > 3-Phenyl-2-[4-[[4-[5-(2-pyridinyl)-1H-1,2,4-triazol-3-yl]-1-piperidinyl]methyl]phenyl]-1,6-Naphthyridin-5(6H)-one

3-Phenyl-2-[4-[[4-[5-(2-pyridinyl)-1H-1,2,4-triazol-3-yl]-1-piperidinyl]methyl]phenyl]-1,6-Naphthyridin-5(6H)-one

Product Name
3-Phenyl-2-[4-[[4-[5-(2-pyridinyl)-1H-1,2,4-triazol-3-yl]-1-piperidinyl]methyl]phenyl]-1,6-Naphthyridin-5(6H)-one
CAS No.
893422-47-4
Chemical Name
3-Phenyl-2-[4-[[4-[5-(2-pyridinyl)-1H-1,2,4-triazol-3-yl]-1-piperidinyl]methyl]phenyl]-1,6-Naphthyridin-5(6H)-one
Synonyms
Akti_2008;Akt1Akt2-IN-17;Akt1/Akt2-IN-1;Akt1/2 inhibitor 1;Akt1 and Akt2-IN-1;Akt-1 and Akt2-IN-1,Akt1 and Akt2IN1,Akt1 and Akt2 IN 1;3-Phenyl-2-[4-[[4-[5-(2-pyridinyl)-1H-1,2,4-triazol-3-yl]-1-piperidinyl]methyl]phenyl]-1,6-Naphthyridin-5(6H)-one;3-phenyl-2-(4-((4-(5-(pyridin-2-yl)-1H-1,2,4-triazol-3-yl)piperidin-1-yl)methyl)phenyl)-1,6-naphthyridin-5(6H)-one;1,6-Naphthyridin-5(6H)-one, 3-phenyl-2-[4-[[4-[5-(2-pyridinyl)-1H-1,2,4-triazol-3-yl]-1-piperidinyl]methyl]phenyl]-
CBNumber
CB62473868
Molecular Formula
C33H29N7O
Formula Weight
539.63
MOL File
893422-47-4.mol
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3-Phenyl-2-[4-[[4-[5-(2-pyridinyl)-1H-1,2,4-triazol-3-yl]-1-piperidinyl]methyl]phenyl]-1,6-Naphthyridin-5(6H)-one Property

Density 
1.285±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO : ≥ 35 mg/mL (64.86 mM)
pka
7.99±0.40(Predicted)
form 
Solid
color 
White to off-white
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene
Product number
CS-5181
Product name
Akt1andAkt2-IN-1
Purity
99.17%
Packaging
5mg
Price
$420
Updated
2021/12/16
ChemScene
Product number
CS-5181
Product name
Akt1andAkt2-IN-1
Purity
99.17%
Packaging
10mg
Price
$600
Updated
2021/12/16
ChemScene
Product number
CS-5181
Product name
Akt1andAkt2-IN-1
Purity
99.17%
Packaging
50mg
Price
$1800
Updated
2021/12/16
ChemScene
Product number
CS-5181
Product name
Akt1andAkt2-IN-1
Purity
99.17%
Packaging
100mg
Price
$2520
Updated
2021/12/16
DC Chemicals
Product number
DC8695
Product name
Akt1andAkt2-IN-1
Purity
>98%
Packaging
1g
Price
$2700
Updated
2021/12/16
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3-Phenyl-2-[4-[[4-[5-(2-pyridinyl)-1H-1,2,4-triazol-3-yl]-1-piperidinyl]methyl]phenyl]-1,6-Naphthyridin-5(6H)-one Chemical Properties,Usage,Production

Biological Activity

Akt1 and Akt2-IN-1 are potent allosteric inhibitors, inhibiting Akt1 (IC50=3.5 nM) and Akt2 (IC50=42 nM).

in vitro

Consistent with the allosteric mode of inhibition, Akt1 and Akt2-IN-1 (Compound 17) is dependent on the PH-domain for Akt inhibition, is selective for Akt1/2 over Akt3 (IC 50 =1900 nM), and is highly selective over other members of the AGC family of kinases (>50 μM vs PKA, PKC, SGK). It has moderate activity in an hERG binding assay (IC 50 =5610 nM) and is a substrate for human P-glycoprotein.

in vivo

Akt1 and Akt2-IN-1 (Compound 17) is well tolerated in at exposures that provide high levels of Akt1 and 2 inhibition in vivo. It has also been shown to inhibit the growth of A2780 tumors in vivo when used as monotherapy. Akt1 and Akt2-IN-1 (Compound 17) has potent inhibitory activity against Akt1 and 2 in vivo in a mouse lung and efficacy in a tumor xenograft model. And it shows good pharmacokinetics in rat with a low clearance of 4.6 mL/min/kg and a half-life of 3.8 h.

target

Akt1

3.5 nM (IC 50 )

Akt2

42 nM (IC 50 )

3-Phenyl-2-[4-[[4-[5-(2-pyridinyl)-1H-1,2,4-triazol-3-yl]-1-piperidinyl]methyl]phenyl]-1,6-Naphthyridin-5(6H)-one Preparation Products And Raw materials

Raw materials

Preparation Products

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3-Phenyl-2-[4-[[4-[5-(2-pyridinyl)-1H-1,2,4-triazol-3-yl]-1-piperidinyl]methyl]phenyl]-1,6-Naphthyridin-5(6H)-one Suppliers

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893422-47-4, 3-Phenyl-2-[4-[[4-[5-(2-pyridinyl)-1H-1,2,4-triazol-3-yl]-1-piperidinyl]methyl]phenyl]-1,6-Naphthyridin-5(6H)-oneRelated Search:

Phenylimidazole 2-Phenylpyridine Pyridine 2,6-Lutidine

  • 3-Phenyl-2-[4-[[4-[5-(2-pyridinyl)-1H-1,2,4-triazol-3-yl]-1-piperidinyl]methyl]phenyl]-1,6-Naphthyridin-5(6H)-one
  • Akti_2008
  • Akt1 and Akt2-IN-1
  • 3-phenyl-2-(4-((4-(5-(pyridin-2-yl)-1H-1,2,4-triazol-3-yl)piperidin-1-yl)methyl)phenyl)-1,6-naphthyridin-5(6H)-one
  • Akt1Akt2-IN-17
  • Akt1/2 inhibitor 1
  • 1,6-Naphthyridin-5(6H)-one, 3-phenyl-2-[4-[[4-[5-(2-pyridinyl)-1H-1,2,4-triazol-3-yl]-1-piperidinyl]methyl]phenyl]-
  • Akt-1 and Akt2-IN-1,Akt1 and Akt2IN1,Akt1 and Akt2 IN 1
  • Akt1/Akt2-IN-1
  • 893422-47-4
  • C33H29N7O