[CAS NO. 1290543-63-3] Nirogacestat (PF-03084014)
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PRODUCTS SPECIFICATIONS [1290543-63-3]
Store
Catalog
SLK-S8018
Brand
Selleck
CAS
1290543-63-3
DESCRIPTION [1290543-63-3]
Overview
| MDL | MFCD19980705 |
|---|---|
| Molecular Weight | 489.64 |
| Molecular Formula | C27H41F2N5O |
| SMILES | FC1=C2C(CC[C@H](N[C@@H](CCC)C(NC3=CN(C(C)(C)CNCC(C)(C)C)C=N3)=O)C2)=CC(F)=C1 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0423 mL | 10.2116 mL | 20.4232 mL |
| 5 mM | 0.4085 mL | 2.0423 mL | 4.0846 mL |
| 10 mM | 0.2042 mL | 1.0212 mL | 2.0423 mL |
| 50 mM | 0.0408 mL | 0.2042 mL | 0.4085 mL |
Description
Nirogacestat (PF-03084014, PF-3084014) is a selective inhibitor with of 6.2 nM in a cell-free assay. Nirogacestat (PF-03084014, PF-3084014) induces . Phase 2.
Targets
| Secretase [1] (cell-free assay) |
| 6.2 nM |
In vitro
PF-03084014 inhibits Notch receptor cleavage in cellular assays using HPB-ALL cells that harbor mutations in both the heterodimerization and PEST domains in Notch1with IC50 of 13.3 nM. PF-03084014 downregulates Notch target genes Hes-1, and cMyc expression in HPB-ALL cells with IC50 of <1 nM and 10 nM, respectively. PF-03084014 inhibits cell growth of a subset of human T-ALL cell lines (HPB-ALL, DND-41, TALL-1,and Sup-T1) through induction of cell cycle arrest and apoptosis with IC50s of 30-100 nM.
PF-03084014 reduces proliferation of HUVECs with IC50 of 0.5 μM, and decreases the lumen formation with an IC50 value of 50 nM. PF-03084014 (1 μM) has no antiproliferative effect in MX1 cells; however, it inhibits migration by 95%.
In vivo
PF-03084014 orally administrated in a single dose of 200 mg/kg, causes maximal NICD inhibition for ∼80% in xenograft HPB-ALL tumors. PF-03084014 shows robust antitumor activity in this mode with a maximal tumor growth inhibition of ∼ 92% at dose of 150 mg/kg, accompanied by a significant reduction of NICD/Notch1, tumor mitotic index (Ki67), and apoptosis (activated caspase-3) staining.
PF-03084014 (120 mg/kg) induces apoptosis, antiproliferation, reduces tumor cell self-renewal ability, impaires tumor vasculature, and decreases metastasis activity in breast cancer HCC1599 tumor-bearing mice. PF-03084014 treatment displays significant antitumor activity in various types of the breast xenograft models with TGI value of at least 50%.
References
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