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
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
N-Bromosuccinimide Price
- Product number
- CS-5181
- Product name
- Akt1andAkt2-IN-1
- Purity
- 99.17%
- Packaging
- 5mg
- Price
- $420
- Updated
- 2021/12/16
- Product number
- CS-5181
- Product name
- Akt1andAkt2-IN-1
- Purity
- 99.17%
- Packaging
- 10mg
- Price
- $600
- Updated
- 2021/12/16
- Product number
- CS-5181
- Product name
- Akt1andAkt2-IN-1
- Purity
- 99.17%
- Packaging
- 50mg
- Price
- $1800
- Updated
- 2021/12/16
- Product number
- CS-5181
- Product name
- Akt1andAkt2-IN-1
- Purity
- 99.17%
- Packaging
- 100mg
- Price
- $2520
- Updated
- 2021/12/16
- Product number
- DC8695
- Product name
- Akt1andAkt2-IN-1
- Purity
- >98%
- Packaging
- 1g
- Price
- $2700
- Updated
- 2021/12/16
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
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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