1. Neuronal Signaling
    Stem Cell/Wnt
  2. γ-secretase
    Notch

RO4929097 

Cat. No.: HY-11102 Purity: 98.02%
Data Sheet SDS Handling Instructions

RO4929097 is a γ secretase inhibitor with 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
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $121 In-stock
5 mg $110 In-stock
10 mg $200 In-stock
50 mg $590 In-stock
100 mg $1050 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

    RO4929097 purchased from MCE. Usage Cited in: ACS Med Chem Lett. 2015 Jun 22;6(8):948-52.

    Combination treatment. (a) Comparison of AZD-8055 and ABT-263 treatment in all cell lines. Red indicates sensitivity, while blue indicates resistance. (b) Depiction of synergism where the values shown are excess over Bliss Independence, a prediction of inhibition without synergism. Increased synergism is evident by an increased number, shown in red, while negative numbers in blue represent an antagonistic effect.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    RO4929097 is a γ secretase inhibitor with IC50 of 4 nM, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively.

    IC50 & Target

    IC50: 4 nM (γ secretase)

    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].

    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].

    Clinical Trial
    NCT Number Sponsor Condition Start Date Phase
    NCT01175343 National Cancer Institute (NCI) Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Stage IV Fallopian Tube Cancer|Stage IV Ovarian Cancer|Stage IV Primary Peritoneal Cancer July 2010 Phase 2
    NCT01141569 National Cancer Institute (NCI) Clear Cell Renal Cell Carcinoma|Recurrent Renal Cell Carcinoma|Stage IV Renal Cell Cancer June 2010 Phase 2
    NCT01198535 National Cancer Institute (NCI) Colon Mucinous Adenocarcinoma|Colon Signet Ring Cell Adenocarcinoma|Rectal Mucinous Adenocarcinoma|Rectal Signet Ring Cell Adenocarcinoma|Recurrent Colon Carcinoma|Recurrent Rectal Carcinoma|Stage IVA Colon Cancer|Stage IVA Rectal Cancer|Stage IVB Colon Cancer|Stage IVB Rectal Cancer September 2010 Phase 1
    NCT01232829 National Cancer Institute (NCI) Adenocarcinoma of the Pancreas|Recurrent Pancreatic Cancer|Stage IV Pancreatic Cancer October 2010 Phase 2
    NCT01154452 National Cancer Institute (NCI) Adult Alveolar Soft Part Sarcoma|Adult Angiosarcoma|Adult Desmoplastic Small Round Cell Tumor|Adult Epithelioid Hemangioendothelioma|Adult Epithelioid Sarcoma|Adult Extraskeletal Myxoid Chondrosarcoma|Adult Extraskeletal Osteosarcoma|Adult Fibrosarcoma|Adult Leiomyosarcoma|Adult Liposarcoma|Adult Malignant Mesenchymoma|Adult Malignant Peripheral Nerve Sheath Tumor|Adult Rhabdomyosarcoma|Adult Synovial Sarcoma|Adult Unclassified Pleomorphic Sarcoma|Chondrosarcoma|Clear Cell Sarcoma of the Kidney| June 2010 Phase 1|Phase 2
    NCT01238133 National Cancer Institute (NCI) Estrogen Receptor Negative|HER2/Neu Negative|Progesterone Receptor Negative|Stage IIA Breast Cancer|Stage IIB Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Triple-Negative Breast Carcinoma December 2010 Phase 1
    NCT01131234 National Cancer Institute (NCI) Adult Anaplastic Astrocytoma|Adult Anaplastic Ependymoma|Adult Anaplastic Oligodendroglioma|Adult Brain Stem Glioma|Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Adult Mixed Glioma|Adult Solid Neoplasm|Male Breast Carcinoma|Recurrent Adult Brain Neoplasm|Recurrent Breast Carcinoma|Recurrent Colon Carcinoma|Recurrent Melanoma|Recurrent Non-Small Cell Lung Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Ovarian Germ Cell Tumor|Recurrent Pancreatic Carcinoma|Recurrent Rectal Ca May 2010 Phase 1
    NCT01120275 National Cancer Institute (NCI) Acral Lentiginous Malignant Melanoma|Lentigo Maligna Malignant Melanoma|Nodular Malignant Melanoma|Recurrent Melanoma|Solar Radiation-related Skin Melanoma|Stage IV Melanoma|Superficial Spreading Malignant Melanoma October 2010 Phase 2
    NCT01122901 National Cancer Institute (NCI) Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Recurrent Adult Brain Tumor December 2010 Phase 2
    NCT01193881 National Cancer Institute (NCI) Recurrent Non-Small Cell Lung Carcinoma|Stage IV Non-Small Cell Lung Cancer August 2010 Phase 1
    NCT01116687 National Cancer Institute (NCI) Recurrent Colon Cancer|Recurrent Rectal Cancer|Stage IV Colon Cancer|Stage IV Rectal Cancer May 2010 Phase 2
    NCT01088763 National Cancer Institute (NCI) Childhood Atypical Teratoid/Rhabdoid Tumor|Childhood Central Nervous System Choriocarcinoma|Childhood Central Nervous System Germinoma|Childhood Central Nervous System Mixed Germ Cell Tumor|Childhood Central Nervous System Teratoma|Childhood Central Nervous System Yolk Sac Tumor|Childhood Choroid Plexus Tumor|Childhood Craniopharyngioma|Childhood Ependymoblastoma|Childhood Grade I Meningioma|Childhood Grade II Meningioma|Childhood Grade III Meningioma|Childhood Infratentorial Ependymoma|Childhoo March 2010 Phase 1
    NCT01193868 National Cancer Institute (NCI)|M.D. Anderson Cancer Center Recurrent Non-small Cell Lung Cancer|Stage IIIB Non-small Cell Lung Cancer|Stage IV Non-small Cell Lung Cancer September 2010 Phase 2
    NCT01216787 National Cancer Institute (NCI) Stage IIIB Melanoma|Stage IIIC Melanoma|Stage IV Melanoma September 2010 Phase 2
    NCT01251172 National Cancer Institute (NCI) DS Stage I Plasma Cell Myeloma|DS Stage II Plasma Cell Myeloma|DS Stage III Plasma Cell Myeloma|Refractory Plasma Cell Myeloma December 2010 Phase 2
    NCT01071564 National Cancer Institute (NCI) Estrogen Receptor Negative|HER2/Neu Negative|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer|Triple-Negative Breast Carcinoma November 2009 Phase 1
    NCT01217411 National Cancer Institute (NCI) Estrogen Receptor-negative Breast Cancer|Extensive Stage Small Cell Lung Cancer|HER2-negative Breast Cancer|HER2-positive Breast Cancer|Male Breast Cancer|Recurrent Breast Cancer|Recurrent Melanoma|Recurrent Non-small Cell Lung Cancer|Recurrent Small Cell Lung Cancer|Stage IV Breast Cancer|Stage IV Melanoma|Stage IV Non-small Cell Lung Cancer|Tumors Metastatic to Brain|Unspecified Adult Solid Tumor, Protocol Specific October 2010 Phase 1|Phase 2
    NCT01158274 National Cancer Institute (NCI) Adult Grade III Lymphomatoid Granulomatosis|Adult Nasal Type Extranodal NK/T-cell Lymphoma|AIDS-related Diffuse Large Cell Lymphoma|AIDS-related Diffuse Mixed Cell Lymphoma|AIDS-related Diffuse Small Cleaved Cell Lymphoma|AIDS-related Immunoblastic Large Cell Lymphoma|AIDS-related Lymphoblastic Lymphoma|AIDS-related Peripheral/Systemic Lymphoma|AIDS-related Primary CNS Lymphoma|AIDS-related Small Noncleaved Cell Lymphoma|Anaplastic Large Cell Lymphoma|Angioimmunoblastic T-cell Lymphoma|Cutaneous June 2010 Phase 1
    NCT01269411 National Cancer Institute (NCI) Adult Anaplastic Oligodendroglioma|Adult Brain Stem Glioma|Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Adult Mixed Glioma|Recurrent Adult Brain Tumor July 2011 Phase 1
    NCT01151449 National Cancer Institute (NCI) Estrogen Receptor-negative Breast Cancer|HER2-negative Breast Cancer|Male Breast Cancer|Progesterone Receptor-negative Breast Cancer|Recurrent Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer|Triple-negative Breast Cancer June 2010 Phase 2
    NCT01096355 National Cancer Institute (NCI) Unspecified Adult Solid Tumor, Protocol Specific February 2010 Phase 1
    NCT01270438 National Cancer Institute (NCI) Adenocarcinoma of the Colon|Adenocarcinoma of the Rectum|Recurrent Colon Cancer|Recurrent Rectal Cancer|Stage IVA Colon Cancer|Stage IVA Rectal Cancer|Stage IVB Colon Cancer|Stage IVB Rectal Cancer December 2010 Phase 2
    NCT01145456 National Cancer Institute (NCI) Adenocarcinoma of the Pancreas|Recurrent Pancreatic Cancer|Stage III Pancreatic Cancer|Stage IV Pancreatic Cancer|Unspecified Adult Solid Tumor, Protocol Specific June 2010 Phase 1
    NCT01198184 National Cancer Institute (NCI) Endometrial Papillary Serous Carcinoma|Recurrent Endometrial Carcinoma|Recurrent Renal Cell Cancer|Stage III Endometrial Carcinoma|Stage III Renal Cell Cancer|Stage IV Endometrial Carcinoma|Stage IV Renal Cell Cancer|Unspecified Adult Solid Tumor, Protocol Specific August 2010 Phase 1
    NCT01196416 National Cancer Institute (NCI) Recurrent Melanoma|Stage IV Skin Melanoma August 2010 Phase 1|Phase 2
    NCT01192763 National Cancer Institute (NCI) Adenocarcinoma of the Pancreas|Stage IA Pancreatic Cancer|Stage IB Pancreatic Cancer|Stage IIA Pancreatic Cancer|Stage IIB Pancreatic Cancer August 2010 Phase 1
    NCT01149356 National Cancer Institute (NCI) Estrogen Receptor Positive|HER2/Neu Negative|Male Breast Carcinoma|Recurrent Breast Carcinoma|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer October 2010 Phase 1
    NCT01119599 National Cancer Institute (NCI) Acoustic Schwannoma|Adult Anaplastic (Malignant) Meningioma|Adult Anaplastic Astrocytoma|Adult Anaplastic Ependymoma|Adult Brain Stem Glioma|Adult Choroid Plexus Neoplasm|Adult Craniopharyngioma|Adult Diffuse Astrocytoma|Adult Ependymoblastoma|Adult Ependymoma|Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Adult Grade I Meningioma|Adult Grade II Meningioma|Adult Medulloblastoma|Adult Mixed Glioma|Adult Myxopapillary Ependymoma|Adult Oligodendroglioma|Adult Papillary Meningiom May 2010 Phase 1
    NCT01200810 National Cancer Institute (NCI) Adenocarcinoma of the Prostate|Recurrent Prostate Cancer|Stage IV Prostate Cancer August 2010 Phase 2
    NCT01070927 Hoffmann-La Roche Non-Squamous Non-Small Cell Lung Cancer January 2010 Phase 2
    NCT01236586 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Lymphoma|Brain Neoplasms|Sarcoma|Osteosarcoma|Wilm's Tumor October 8, 2010 Phase 1
    NCT01189240 National Cancer Institute (NCI) Adult Anaplastic Astrocytoma|Adult Anaplastic Oligodendroglioma|Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Recurrent Adult Brain Tumor December 2010 Phase 1|Phase 2
    NCT01208441 National Cancer Institute (NCI) Estrogen Receptor-positive Breast Cancer|HER2-negative Breast Cancer|Progesterone Receptor-positive Breast Cancer|Stage II Breast Cancer|Stage IIIA Breast Cancer November 2010 Phase 1
    NCT01218620 National Cancer Institute (NCI) Adult Solid Neoplasm September 2010 Phase 1
    View MoreCollapse
    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) 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
    10 mM 0.2130 mL 1.0652 mL 2.1304 mL
    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]

    RO4929097 is formulated as a suspension in 1.0% Klucel in water with 0.2% Tween 80.

    RO4929097 is formulated as a suspension in 1.0% Klucel in water with 0.2% Tween 80 for oral administration. 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
    Molecular Weight

    469.4

    Formula

    C₂₂H₂₀F₅N₃O₃

    CAS No.

    847925-91-1

    Storage

    Powder4°C, stored under nitrogen

    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 49 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product name

     

    Salutation

    Applicant name *

     

    Email address *

    Phone number

     

    Organization name *

    Country *

     

    Requested quantity *

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    RO4929097
    Cat. No.:
    HY-11102
    Quantity: