2. Neuronal Signaling Stem Cell/Wnt Apoptosis
  3. γ-secretase Apoptosis
  4. Nirogacestat dihydrobromide

Nirogacestat dihydrobromide  (Synonyms: PF-3084014 dihydrobromide; PF-03084014 dihydrobromide)

Cat. No.: HY-15185B Pureza: 99.81% ee.: 100%
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Nirogacestat dihydrobromide (PF-3084014 dihydrobromide) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC50 of 6.2 nM. Inhibition of Notch signaling by Nirogacestat dihydrobromide while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers.

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No. CAS : 1962925-29-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 En stock
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Revisión del cliente

Based on 15 publication(s) in Google Scholar

Other Forms of Nirogacestat dihydrobromide:

Nirogacestat dihydrobromide Related Antibodies

Top Publications Citing Use of Products

    Nirogacestat dihydrobromide purchased from MedChemExpress. Usage Cited in: Nat Med. 2023 Sep;29(9):2295-2306.  [Abstract]

    Soluble BCMA was measured from the supernatant of K562 cell line cultures using the sBCMA DuoSet kit. The cell lines were cultured with the γ-secretase inhibitor Nirogacestat (PF-3084014) (6.2 nM).

    Nirogacestat dihydrobromide purchased from MedChemExpress. Usage Cited in: Neuron. 2023 Jun 21;111(12):1898-1913.e5.  [Abstract]

    Treatment with γ-secretase inhibitor Nirogacestat (PF03084014) (1 mM) increased α-CTF to a level similar to ApoE CT treatment in HEK 293T cells.

    Nirogacestat dihydrobromide purchased from MedChemExpress. Usage Cited in: Neuron. 2023 Jun 21;111(12):1898-1913.e5.  [Abstract]

    Aβ40 production was measured from the incubation of purified β-CTF (0.1 mM) alone or co-incubation with γ-secretase (0.001 mM) after treatment with vehicle or Nirogacestat (PF03084014) (10 mM).

    Nirogacestat dihydrobromide purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2021 Mar 8;39(3):380-393.e8.  [Abstract]

    Exposure to the gamma-secretase inhibitor Nirogacestat (PF308414) (6.2 nM), which targeted NOTCH signaling, led to decreased viability of mut-Ikzf3 CLL cells.

    Nirogacestat dihydrobromide purchased from MedChemExpress. Usage Cited in: Int J Oncol. 2018 Jul;53(1):99-112.  [Abstract]

    The expression of E-cadherin, N-cadherin and Snail in Enza-R cells is examined by western blot analysis. The cells are transfected with Ad-GFP or Ad-HepaCAM for 72 h and treated with 5 μM PF-3084014 for 48 h. GAPDH served as a loading control.

    Nirogacestat dihydrobromide purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2017 Jul;9(7):950-966.  [Abstract]

    Turnover of endogenous CD74 P8 is inhibited by RO4929079 and BMS-906024. Cell lysate Western blot of A20 cells treated with GSIs is developed with In-1 antibody. MK-0752 and Semagacestat tests used the same control lane (0 nM).

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    Descripciòn

    Nirogacestat dihydrobromide (PF-3084014 dihydrobromide) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC50 of 6.2 nM. Inhibition of Notch signaling by Nirogacestat dihydrobromide while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers[1].

    In Vitro

    The IC50 of Nirogacestat (PF-03084014) for γ-secretase enzyme inhibition in cell-free assay for Aβ production using detergent solubilized membranes derived from HeLa cells is determined to be 6.2 nM. When tested for inhibition of Notch receptor cleavage in cellular assays using HPB-ALL cells that harbor mutations in both the heterodimerization and PEST domains in Notch1, the cell IC50 is determined to be 13.3 nM. Nirogacestat causes a significant increase in caspase-3 activities in HPB-ALL and TALL-1 cells as well as an induction of cleaved PARP and cleaved caspase-3 after a 7-day treatment[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Nirogacestat dihydrobromide Related Antibodies
    In Vivo

    Nirogacestat (PF-03084014) shows robust antitumor activity in this model on 14-day twice daily dosing. Tumor growth inhibition is dose dependent, with maximal tumor growth inhibition of ~92% obtained at high dose levels (150 mg/kg). In tumor growth inhibition studies where mice receive repetitive twice daily dosing for more than a week, Nirogacestat is well tolerated at dose levels below 100 mg/kg as no significant weight loss, morbidity, or mortality is observed. When the dose is increased to 150 mg/kg, however, mice have diarrhea and show weight loss (10-15%) approximately 10 days after compound administration. The body weight of treated animals usually returns to normal if dosing holidays are given, suggesting that the toxicity of Nirogacestat is reversible[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Peso molecular

    651.47

    Fòrmula

    C27H43Br2F2N5O
    No. CAS
    Appearance

    Solid

    Color

    White to yellow

    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.Br.Br
    Envío

    Room temperature in continental US; may vary elsewhere.
    Almacenamiento

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvente y solubilidad
    In Vitro: 

    DMSO : 80 mg/mL (122.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.5350 mL 7.6750 mL 15.3499 mL
    5 mM 0.3070 mL 1.5350 mL 3.0700 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Calculadora de molaridad

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

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    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

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    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    Pureza y Documentación

    Purity: 99.81% ee.: 100%

    SDS (252 KB)

    COA (250 KB) HNMR (330 KB) RP-HPLC (222 KB) NP-HPLC (151 KB) MS (70 KB)

    Instrucciones de manejo (2659 KB)
    Referencias

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.5350 mL 7.6750 mL 15.3499 mL 38.3748 mL
    5 mM 0.3070 mL 1.5350 mL 3.0700 mL 7.6750 mL
    10 mM 0.1535 mL 0.7675 mL 1.5350 mL 3.8375 mL
    15 mM 0.1023 mL 0.5117 mL 1.0233 mL 2.5583 mL
    20 mM 0.0767 mL 0.3837 mL 0.7675 mL 1.9187 mL
    25 mM 0.0614 mL 0.3070 mL 0.6140 mL 1.5350 mL
    30 mM 0.0512 mL 0.2558 mL 0.5117 mL 1.2792 mL
    40 mM 0.0384 mL 0.1919 mL 0.3837 mL 0.9594 mL
    50 mM 0.0307 mL 0.1535 mL 0.3070 mL 0.7675 mL
    60 mM 0.0256 mL 0.1279 mL 0.2558 mL 0.6396 mL
    80 mM 0.0192 mL 0.0959 mL 0.1919 mL 0.4797 mL
    100 mM 0.0153 mL 0.0767 mL 0.1535 mL 0.3837 mL
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    Nirogacestat dihydrobromide Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Nirogacestat dihydrobromide1962925-29-6PF-3084014 dihydrobromide PF-03084014 dihydrobromideγ-secretaseApoptosisGamma secretaseNotchgastrointestinaltoxicitycancerInhibitorinhibitorinhibit

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    Nombre del producto:
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