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Nirogacestat

CAT: 0804-HY-15185-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-15185-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
Nirogacestat (PF-3084014) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC50 of 6.2 nM. Inhibition of Notch signaling by Nirogacestat while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers[1].
CAS Number
1290543-63-3
Product Name Alternative
PF-3084014
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
Apoptosis; γ-secretase
Type
Reference compound
Related Pathways
Apoptosis; Neuronal Signaling; Stem Cell/Wnt
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/PF-3084014.html
Purity
99.83
Solubility
DMSO : 28.57 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL (ultrasonic; warming; heat to 60°C)
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
Molecular Formula
C27H41F2N5O
Molecular Weight
489.64
Precautions
H302, H315, H319, H335
References & Citations
[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Launched
Citation 01
ACS Appl Mater Interfaces. 2024 Sep 11;16 (36) :47075-47088.|Cancer Cell. 2021 Mar 8;39 (3) :380-393.e8.|EBioMedicine. 2025 Aug 15:119:105879.|EMBO Mol Med. 2017 Jul;9 (7) :950-966.|Int J Oncol. 2018 Jul;53 (1) :99-112.|J Biol Chem. 2019 Jul 19;294 (29) :11276-11285.|J Biol Chem. 2021 Jan-Jun:296:100593.|J Clin Invest. 2020 Feb 3;130 (2) :612-624.|Mol Immunol. 2018 Jul:99:191-198.|Nat Biotechnol. 2024 Nov 25.|Nat Mater. 2025 Feb 17.|Nat Med. 2023 Sep;29 (9) :2295-2306.|Neuron. 2023 Jun 21;111 (12) :1898-1913.e5.|Research Square Print. 2023 Mar 20.|bioRxiv. 2025 May 28.

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