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PF-03084014 (Nirogacestat) is a potent and selective gamma secretase (GS) inhibitor with potential antitumor activity. PF-03084014 binds to GS, blocking proteolytic activation of Notch receptors. 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.
In vivo, PF-03084014 (Nirogacestat) orally administrated in a single dose of 200 mg/kg, causes maximal NICD inhibition for ∼80% in xenograft HPB-ALL tumors. 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%.
| Molecular Weight | 489.64 |
| Formula | C27H41F2N5O |
| CAS Number | 1290543-63-3 |
| Solubility (25°C) | DMSO 25 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Gamma-secretase/Beta-secretase Products |
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| DAPT
DAPT (GSI-IX) is a γ-secretase inhibitor with IC50 values of 115 and 200 nM for total Aβ and Aβ42 respectively. DAPT inhibits the activation of Notch 1 signaling. |
| BMS-708163
BMS-708163 (Avagacestat) is a selective γ-secretase inhibitor (IC50 = 0.3 nM). |
| RO4929097
RO4929097 is a potent and selective inhibitor of γ-secretase and as a result is able to inhibit Notch pathway signaling. |
| MK-0752
MK-0752 is a potent, oral inhibitor of γ-secretase with IC50 of 5 nM in human SH-SY5Y cells. |
| LY-411575
LY-411575 is potent and selective small molecule γ-secretase inhibitor with IC50 of 0.1 nM for APP23 and APP51/16 primary neurons. |
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