2. Neuronal Signaling Stem Cell/Wnt
  3. γ-secretase Notch
  4. RO4929097

RO4929097 (RG-4733) is an orally active γ secretase inhibitor with an IC50 of 4 nM, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively.

For research use only. We do not sell to patients.

RO4929097 Chemical Structure

RO4929097 Chemical Structure

CAS No. : 847925-91-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 17 publication(s) in Google Scholar

RO4929097 Related Antibodies

Top Publications Citing Use of Products

    RO4929097 purchased from MedChemExpress. Usage Cited in: FASEB J. 2017 Sep;31(9):3774-3786.  [Abstract]

    Western blot analysis of E-cadherin, vimentin, Slug, and Twist1 in BGC823 cells treated with RO4929097 in addition to miR-2392 inhibition.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    RO4929097 (RG-4733) is an orally active γ secretase inhibitor with an IC50 of 4 nM, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively[1].

    IC50 & Target

    IC50: 4 nM (γ secretase)[1]
    Cellular Effect
    Cell Line Type Value Description References
    HEK293 EC50
    14 nM
    Compound: 12; RO4929097
    Inhibition of gamma secretase in HEK293 cells expressing APP695 assessed as reduction in amyloid beta (1 to 40 residues) by ELISA
    Inhibition of gamma secretase in HEK293 cells expressing APP695 assessed as reduction in amyloid beta (1 to 40 residues) by ELISA
    		[PMID: 27045975]
    HEK293 EC50
    5 nM
    Compound: 12; RO4929097
    Inhibition of gamma secretase mediated Notch1 signaling in HEK293 cells expressing truncated human Notch1 by luciferase reporter gene assay
    Inhibition of gamma secretase mediated Notch1 signaling in HEK293 cells expressing truncated human Notch1 by luciferase reporter gene assay
    		[PMID: 27045975]
    In Vitro

    RO4929097 inhibits the production of ICN reducing the expression of the downstream Notch target, Hes1, producing a less transformed morphology in A549 cells. RO4929097 inhibits Notch processing in human tumor-derived cells[1].RO4929097 (1 μM) inhibits the growth of breast cancer cells, and the inhibition is 20% for SUM149 and 10% for SUM190 cells. RO4929097 does not have a marked effect in invasiveness of SUM149 cells. RO4929097 significantly reduces colony formation by both cell lines with the effect being more notable in SUM149 than by SUM190 cells[2]. RO4929097 inhibits proliferation, anchorage independent growth, and sphere formation of primary melanoma cells in vitro[3].

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

    RO4929097 Related Antibodies
    In Vivo

    RO4929097 (3-60 mg/kg, p.o.) results in significant tumor growth inhibition in nude mice bearing A549 NSCLC xenografts, compared with vehicle-treated animals. When mice are treated with 60 mg/kg RO4929097 twice daily with the 7+/14- schedule, treatment initially causes regression of established A549 tumors[1]. RO4929097 impairs the growth of primary melanoma cells in vivo. The percentage of secondary tumors formed by RO4929097-treated cells is lower; the secondary tumors formed by RO4929097-treated cells are smaller; a significant delay in tumor formation by the RO4929097-treated cells compared to the vehicle-treated ones is observed in mice injected with 104 cells in vivo[3].

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

    469.40

    Formula

    C22H20F5N3O3
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C(C)(C(NCC(F)(C(F)(F)F)F)=O)C)N[C@H]1C2=CC=CC=C2C3=CC=CC=C3NC1=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, stored under nitrogen

    *In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 49 mg/mL (104.39 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1304 mL 10.6519 mL 21.3038 mL
    5 mM 0.4261 mL 2.1304 mL 4.2608 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, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Volume
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    Molecular Weight *

    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:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.33 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.33 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.01%

    SDS (393 KB)

    COA (257 KB) LCMS (94 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [2]

    The IBC cell lines SUM149 and SUM190 are seeded at a density of 5 × 104 cells. The next day, they are treated with vehicle or increasing doses of RO4929097, ranging from 0.1 nM to 10 μM. After 72 hrs, cells are trypsinized and viable cells counted with a hemocytometer.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice: RO4929097-treated mice are orally dosed with suspensions at 3 to 60 mg/kg RO4929097 according to the indicated regimens. In the Calu-6 xenograft model, RO4929097 is dosed at 60 mg/kg/d every other week for 4 weeks (7+/7- × 2 cycles). For all other xenograft models, RO4929097 is dosed once daily at 10 mg/kg for 21 days. Statistical analysis is determined by Mann-Whitney rank-sum test, one-way ANOVA, and post hoc Bonferroni t test. Differences between groups are considered significant when P ≤ 0.05. A549 tumors from vehicle-treated and selected RO4929097-treated groups are collected and fixed in 10% zinc-formalin overnight, processed, paraffin-embedded, sectioned at 5 μM, and stained with H&E for histopathology assessment. An Olympus BX51 microscope (×40 objective) mounted with a Nikon DS-Fi1 using the NIS-Elements F2.20 program collected the histology pictures. For Western blot analysis, three A549 tumors from each group, 7 (60 mg/kg) or 21 days (3 and 30 mg/kg), are flash-frozen. Collagen type V is detected using the H-200 antibody at a dilution of 1:1,000, and MFAP5 is detected using the antibody at a dilution of 1:1,000.

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

    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, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1304 mL 10.6519 mL 21.3038 mL 53.2595 mL
    5 mM 0.4261 mL 2.1304 mL 4.2608 mL 10.6519 mL
    10 mM 0.2130 mL 1.0652 mL 2.1304 mL 5.3259 mL
    15 mM 0.1420 mL 0.7101 mL 1.4203 mL 3.5506 mL
    20 mM 0.1065 mL 0.5326 mL 1.0652 mL 2.6630 mL
    25 mM 0.0852 mL 0.4261 mL 0.8522 mL 2.1304 mL
    30 mM 0.0710 mL 0.3551 mL 0.7101 mL 1.7753 mL
    40 mM 0.0533 mL 0.2663 mL 0.5326 mL 1.3315 mL
    50 mM 0.0426 mL 0.2130 mL 0.4261 mL 1.0652 mL
    60 mM 0.0355 mL 0.1775 mL 0.3551 mL 0.8877 mL
    80 mM 0.0266 mL 0.1331 mL 0.2663 mL 0.6657 mL
    100 mM 0.0213 mL 0.1065 mL 0.2130 mL 0.5326 mL
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    RO4929097 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:

    RO4929097847925-91-1RG-4733RO 4929097RO-4929097RG4733RG 4733γ-secretaseNotchGamma secretaseInhibitorinhibitorinhibit

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