893422-47-4
893422-47-4 structure
- Name: Akt1 and Akt2-IN-1
- Chemical Name: 3-Phenyl-2-[4-({4-[3-(2-pyridinyl)-1H-1,2,4-triazol-5-yl]-1-piperidinyl}methyl)phenyl]-1,6-naphthyridin-5(6H)-one
- CAS Number: 893422-47-4
- Molecular Formula: C33H29N7O
- Molecular Weight: 539.63000
- Catalog: Research Areas Cancer
- Create Date: 2018-04-18 02:17:44
- Modify Date: 2024-01-13 20:55:05
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Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 (IC50=3.5 nM) and Akt2 (IC50=42 nM), with potent and balanced activity.
| Name | 3-Phenyl-2-[4-({4-[3-(2-pyridinyl)-1H-1,2,4-triazol-5-yl]-1-piperidinyl}methyl)phenyl]-1,6-naphthyridin-5(6H)-one |
|---|---|
| Synonyms |
1,6-Naphthyridin-5(6H)-one, 3-phenyl-2-[4-[[4-[3-(2-pyridinyl)-1H-1,2,4-triazol-5-yl]-1-piperidinyl]methyl]phenyl]-
3-Phenyl-2-[4-({4-[3-(2-pyridinyl)-1H-1,2,4-triazol-5-yl]-1-piperidinyl}methyl)phenyl]-1,6-naphthyridin-5(6H)-one Akt1 and Akt2-IN-1 |
| Description | Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 (IC50=3.5 nM) and Akt2 (IC50=42 nM), with potent and balanced activity. |
|---|---|
| Related Catalog | |
| Target |
Akt1:3.5 nM (IC50) Akt2:42 nM (IC50) |
| 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 (IC50=1900 nM), and is highly selective over other members of the AGC family of kinases (>50 μM vs PKA, PKC, SGK). Akt1 and Akt2-IN-1 (Compound 17) has moderate activity in an hERG binding assay (IC50=5610 nM) and is a substrate for human P-glycoprotein[1]. |
| 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. Akt1 and Akt2-IN-1 (Compound 17) 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. Akt1 and Akt2-IN-1 (Compound 17) shows good pharmacokinetics in rat with a low clearance of 4.6 mL/min/kg and a half-life of 3.8 h. Due to the improved cell potency, physical properties, and rodent pharmacokinetics of Akt1 and Akt2-IN-1 (Compound 17), tolerability and Akt inhibition are assessed in mice. Using an acute dosing schedule (IP dosing of 50 mg/kg at times 0, 3, and 8 h), administration of Akt1 and Akt2-IN-1 (Compound 17) is well tolerated in mice and shows high levels of Akt inhibition in mouse lung[1]. |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Molecular Formula | C33H29N7O |
| Molecular Weight | 539.63000 |
| Exact Mass | 539.24300 |
| PSA | 103.45000 |
| LogP | 3.59 |
| Index of Refraction | 1.666 |
| Storage condition | 2-8℃ |