Nirogacestat (PF-03084014) | γ-secretase inhibitor | Probechem Biochemicals

Chemical Structure : Nirogacestat

CAS No.: 1290543-63-3

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Nirogacestat (PF-03084014, PF 03084014)

货号: 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).

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5 mg	￥880	In stock
10 mg	￥1380	In stock
25 mg	￥2480	In stock
50 mg	￥3980	In stock
100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	489.656
分子式	C27H41F2N5O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
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

参考文献

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.

Nirogacestat (PF-03084014, PF 03084014)

生物&药学活性

物理化学性质&存储条件

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Nirogacestat (PF-03084014, PF 03084014)

生物&药学活性

物理化学性质&存储条件

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