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 manufacturers
- Akt1 and Akt2-IN-1
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- $347.00 / 5mg
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2024-10-28
- CAS:893422-47-4
- Min. Order:
- Purity:
- Supply Ability: 10g
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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 Basic information |
| 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 | | Synonyms: | 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 | | CAS: | 893422-47-4 | | MF: | C33H29N7O | | MW: | 539.63 | | EINECS: | | | Product Categories: | | | 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 Structure](CAS/GIF/893422-47-4.gif) |
| | 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 |
| 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 |
| | 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 Usage And Synthesis |
| 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 |
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