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Nirogacestat

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].

Product Specifications

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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