![]() 6-[4-(1-Aminocyclobutyl)phenyl]-5-phenyl-3-pyridinecarboxamide structure
|
Common Name | 6-[4-(1-Aminocyclobutyl)phenyl]-5-phenyl-3-pyridinecarboxamide | ||
---|---|---|---|---|
CAS Number | 1357158-81-6 | Molecular Weight | 343.422 | |
Density | 1.2±0.1 g/cm3 | Boiling Point | 496.4±45.0 °C at 760 mmHg | |
Molecular Formula | C22H21N3O | Melting Point | N/A | |
MSDS | N/A | Flash Point | 254.0±28.7 °C |
Use of 6-[4-(1-Aminocyclobutyl)phenyl]-5-phenyl-3-pyridinecarboxamideAKT-IN-1 is an allosteric AKT inhibitor with an IC50 of 1.042 μM. |
Name | 6-(4-(1-aminocyclobutyl)phenyl)-5-phenylnicotinamide |
---|---|
Synonym | More Synonyms |
Description | AKT-IN-1 is an allosteric AKT inhibitor with an IC50 of 1.042 μM. |
---|---|
Related Catalog | |
Target |
IC50: 1.042 μM (AKT)[1] |
In Vitro | AKT-IN-1 (Compound 26) is able to potently inhibit phosphorylation of AKT in cells at both Thr308 and Ser473, with IC50s of 0.422 and 0.322 μM, respectively. AKT-IN-1 inhibits the phosphorylation of ribosomal protein S6, a downstream effector of the PI3K-AKT pathway. AKT-IN-1 potently inhibits the phosphorylation of PRAS40[1]. |
In Vivo | The effects of AKT-IN-1 (Compound 26) in vivo are characterized by measuring the pharmacodynamic activity of AKT-IN-1 in a BT474c breast adenocarcinoma xenograft model. Following acute doses of 100 and 200 mg/kg, AKT-IN-1 potently inhibits the phosphorylation of its downstream substrate GSK3β as well as the phosphorylation of AKT (Ser473), with a potency consistent with its pharmacokinetic profile. The in vivo activity of AKT-IN-1 is further characterized by measuring the effects on the growth of tumor cell xenografts. Continuous (daily) oral dosing of AKT-IN-1 (100 and 200 mg/kg) to nude mice bearing BT474c breast adenocarcinoma xenografts results in inhibition of tumor growth in a dose-dependent manner. When dosed at 200 mg/kg daily, AKT-IN-1 causes significant tumor growth inhibition[1]. |
References |
Density | 1.2±0.1 g/cm3 |
---|---|
Boiling Point | 496.4±45.0 °C at 760 mmHg |
Molecular Formula | C22H21N3O |
Molecular Weight | 343.422 |
Flash Point | 254.0±28.7 °C |
Exact Mass | 343.168457 |
PSA | 82.00000 |
LogP | 2.87 |
Vapour Pressure | 0.0±1.3 mmHg at 25°C |
Index of Refraction | 1.643 |
Storage condition | 2-8℃ |
Water Solubility | Practically insoluble (0.041 g/L) (25 ºC) |
6-[4-(1-Aminocyclobutyl)phenyl]-5-phenylnicotinamide |
3-Pyridinecarboxamide, 6-[4-(1-aminocyclobutyl)phenyl]-5-phenyl- |
6-[4-(1-Aminocyclobutyl)phenyl]-5-phenyl-3-pyridinecarboxamide |
AZD-26 |
AKT-IN-1 |