PF 03084014 - Names and Identifiers
PF 03084014 - Physico-chemical Properties
Molecular Formula | C27H41F2N5O
|
Molar Mass | 489.64 |
Appearance | powder |
Color | white to beige |
Storage Condition | room temp |
Use | Nirogacestat (PF-3084014) is an effective, orally active, reversible, non-competitive selective γ-secretase inhibitor with an IC50 of 6.2 nM. Nirogacestat inhibit Notch signaling pathway while minimizing gastrointestinal toxicity. It can be used to study Notch receptor-dependent tumors. |
Target | γ secretase |
PF 03084014 - Risk and Safety
PF 03084014 - Reference
Reference Show more | 1. Wei P, et al. Evaluation of selective gamma-secretase inhibitor PF-03084014 for its antitumor efficacy and gastrointestinal safety to guide optimal clinical trial design. Mol Cancer Ther. 2010 Jun;9(6):1618-28. |
PF 03084014 - Preparation solution concentration reference
| 1mg | 5mg | 10mg |
---|
1 mM | 2.042 ml | 10.212 ml | 20.423 ml |
5 mM | 0.408 ml | 2.042 ml | 4.085 ml |
10 mM | 0.204 ml | 1.021 ml | 2.042 ml |
5 mM | 0.041 ml | 0.204 ml | 0.408 ml |
Last Update:2024-01-02 23:10:35
PF 03084014 - Cell Experiment
Cell lines: Human T-ALL cell lines HPB-ALL. Concentrations: ~1 μM. Method: Cells are seeded in 96-well plates at 10,000 cells/well in growth media supplemented with 10% fetal bovine serum.Serial dilutions of PF-03084014 are done in DMSO,appropriate controls or designated concentrations of PF-03084014 are added to each well,and cells are incubated at 37℃ for 7 days (final DMSO content 0.1%).Resazurin at a final concentration of 0.1 mg/mL is added to the cells and plates are incubated for 2 to 4 hours.Fluorescent signals are read as emission at 590 nm after excitation at 560 nm. Cell lines:
Last Update:2023-08-16 21:32:38
PF 03084014 - Animal Experiment
Animal Models: Human T-cell acute lymphoblastic leukemia xenografts HPB-ALL. Formulation: 0.5% methylcellulose. Dosages: 150 mg/kg,b.i.d. Administration: p.o.
Last Update:2023-08-16 21:32:38
PF 03084014 - Reference Information
biological activity | Nirogacestat (PF-03084014, PF-3084014) is a selective gamma-secretase inhibitor, the IC50 in the cell-free assay was 6.2 nM. Nirogacestat (PF-03084014, PF-3084014) induced apoptosis. Phase 2. |
Target | TargetValue gamma-secretase (cell-free assay) 6.2 nM |
Target | Value |
γ-secretase
(cell-free assay)
| 6.2 nM |
Last Update:2024-04-09 21:04:16