| Identification | Back Directory | [Name]
[1,2,4]Triazolo[1,5-a]pyrimidine-4(7H)-acetamide, 2-(3,6-dihydro-2H-pyran-4-yl)-5-ethyl-6-[4-[(3-hydroxy-2-pyridinyl)carbonyl]-1-piperazinyl]-N-[2-methyl-4-(trifluoromethyl)phenyl]-7-oxo- | [CAS]
2869954-53-8 | [Synonyms]
Werner syndrome RecQ helicase-IN-4
2-(2-(3,6-dihydro-2H-pyran-4-yl)-5-ethyl-6-(4-(3-hydroxypicolinoyl)piperazin-1-yl)-7-oxo-[1,2,4]triazolo[1,5-a]pyrimidin-4(7H)-yl)-N-(2-methyl-4-(trifluoromethyl)phenyl)acetamide
[1,2,4]Triazolo[1,5-a]pyrimidine-4(7H)-acetamide, 2-(3,6-dihydro-2H-pyran-4-yl)-5-ethyl-6-[4-[(3-hydroxy-2-pyridinyl)carbonyl]-1-piperazinyl]-N-[2-methyl-4-(trifluoromethyl)phenyl]-7-oxo- | [Molecular Formula]
C32H33F3N8O5 | [MOL File]
2869954-53-8.mol | [Molecular Weight]
666.65 |
| Chemical Properties | Back Directory | [density ]
1.49±0.1 g/cm3(Predicted) | [solubility ]
DMSO: Sparingly soluble: 1-10 mg/ml | [form ]
Solid | [pka]
6.20±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Werner syndrome RecQ helicase-IN-4 is a potent and orally active werner syndrome recQ helicase (WRN) inhibitor with an IC50 value of 0.06 μM. Werner syndrome RecQ helicase-IN-4 shows antiproliferative activity. Werner syndrome RecQ helicase-IN-4 shows anticancer activity[1]. | [in vivo]
Werner syndrome RecQ helicase-IN-4 (240 mg/kg; daily for 18 days) shows anticancer activity in mouse[1]. | Animal Model: | Female Crl:NU(NCr)-Foxn1nu -Homozygous nude mice (SW48 xenografts cells)[1] | | Dosage: | 240 mg/kg | | Administration: | P.o.; daily for 18 days | | Result: | Inhibited tumor growth. |
| [References]
[1] Vincent Bordas, et al. Triazolo-pyrimidine analogues for treating diseases connected to the inhibiton of werner syndrome recq helicase (wrn). WO2022249060A1. |
|
|