| Identification | Back Directory | [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]
893422-47-4 | [Synonyms]
Akti_2008
Akt1Akt2-IN-17
Akt1/2 inhibitor 1
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]- | [Molecular Formula]
C33H29N7O | [MDL Number]
MFCD13184803 | [MOL File]
893422-47-4.mol | [Molecular Weight]
539.63 |
| Chemical Properties | Back Directory | [density ]
1.285±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : ≥ 35 mg/mL (64.86 mM) | [form ]
Solid | [pka]
7.99±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Akt1/Akt2-IN-1 (Compound 17) is an allosteric inhibitor of Akt1 (IC50=3.5 nM) and Akt2 (IC50=42 nM), with potent and balanced activity[1]. | [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 ) | | [IC 50]
Akt1: 3.5 nM (IC50); Akt2: 42 nM (IC50) | [References]
[1] Bilodeau MT, Allosteric inhibitors of Akt1 and Akt2: a naphthyridinone with efficacy in an A2780 tumor xenograft model. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3178-82. DOI:10.1016/j.bmcl.2008.04.074 |
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