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