Name | VPS34 inhibitor 1 |
Synonyms | Vps Compound 19 VPS34INHIBITOR VPS34 inhibitor PIK-III analogue VPS34 inhibitor 1 Compound 19, PIK-III analogue VPS34 inhibitor 1 (PIK-III analogue) VPS34 inhibitor 1 (Compound 19, PIK-III analogue) 1-((4'-(cyclopropylmethyl)-2-(pyridin-4-ylamino)-[4,5'-bipyrimidin]-2'-yl)amino)-2-methylpropan-2-ol |
CAS | 1383716-46-8 |
Molecular Formula | C21H25N7O |
Molar Mass | 391.47 |
Density | 1.324±0.06 g/cm3(Predicted) |
Boling Point | 676.1±65.0 °C(Predicted) |
pKa | 14.68±0.29(Predicted) |
Storage Condition | -20℃ |
In vitro study | Compound 19 is very selective among lipid and protein kinases. compound 19 was able to block the degradation of autophagy substrates p62, NCOA4, NBR1, NDP52 and fth1. Treatment of cells with compound 19 was able to increase lipidated and non-lipidated forms of lc3. |
In vivo study | Detection of the pharmacokinetic type of compound 19 in C57BL/6 mice. After oral administration of 10 mg/kg Compound 19 in mice, the Compound is rapidly absorbed in the body with a moderate level of systemic clearance (30 mL/min/kg, hepatic blood flow of about 33%), good oral bioavailability (F% = 47). Based on these pharmacokinetic parameters and cellular activity, compound 19 is a suitable candidate for in vivo studies. Oral administration of 50 mg/kg Compound 19 once every two days for 7 days in mice resulted in a time-dependent decrease in LC3-II accumulation and autophagy. In Vivo, Compound 19 inhibits the autophagy response. |