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Chemical Structure : Nirogacestat
CAS No.: 1290543-63-3
Catalog No.: PC-49410Not For Human Use, Lab Use Only.
Nirogacestat (PF-03084014) is a potent, noncompetitive, and selective gamma-secretase inhibitor, reduces amyloid-beta (Abeta) production with in vitro IC50 of 1.2 nM (whole-cell assay) to 6.2 nM (cell-free assay).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $258 | In stock | |
| 50 mg | $458 | In stock | |
| 100 mg | $758 | In stock | |
| 1 g | Get quote |
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Nirogacestat (PF-03084014) is a potent, noncompetitive, and selective gamma-secretase inhibitor, reduces amyloid-beta (Abeta) production with in vitro IC50 of 1.2 nM (whole-cell assay) to 6.2 nM (cell-free assay).
PF-03084014 inhibits Notch-related T- and B-cell maturation in an in vitro thymocyte assay with an EC(50) of 2.1 uM.
PF-03084014 inhibited gamma-secretase activity was shown by the reduction of endogenous Notch intracellular domain (NICD) levels and by the downregulation of Notch target genes Hes-1 and cMyc in the T-cell acute lymphoblastic leukemia (T-ALL) cell line HPB-ALL.
PF-03084014 caused cell growth inhibition of several T-ALL cell lines via cell cycle arrest and induction of apoptosis.
PF-03084014 treatment also resulted in robust NICD reduction in HBP-ALL xenograft models, exhibited broad antitumor efficacy in Notch-dependent models.
| M.Wt | 489.656 | |
| Formula | C27H41F2N5O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(S)-2-((S)-5,7-difluoro-1,2,3,4-tetrahydronaphthalen-3-ylamino)-N-(1-(2-methyl-1-(neopentylamino)propan-2-yl)-1H-imidazol-4-yl)pentanamide |
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1. Lanz TA, et al. J Pharmacol Exp Ther. 2010 Jul;334(1):269-77.
2. Wei P, et al. Mol Cancer Ther. 2010 Jun;9(6):1618-28.
3. Brodney MA, et al. Bioorg Med Chem Lett. 2011 May 1;21(9):2637-40.
4. Samon JB, et al. Mol Cancer Ther. 2012 Jul;11(7):1565-75.
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