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Signaling Pathway



(RO-4929097; RO 4929097)


RO4929097 Chemical Structure

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.

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10 mM * 1 mL in DMSO $121 In-stock
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Free sample   Apply now  
10 mM * 1 mL in DMSO €119 In-stock
5 mg €108 In-stock
10 mg €196 In-stock
50 mg €578 In-stock
100 mg €1029 In-stock
200 mg Get quote
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Product name: RO4929097
Cat. No.: HY-11102

RO4929097 Data Sheet

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    Purity: 98.02%

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Biological Activity of RO4929097

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 value: 4 nM
Target: γ secretase
in vitro: RO4929097 decreases the amount of Aβ peptides secreted into the culture medium in HEK293 cells with EC50 of 14 nM. RO4929097 strongly inhibits Notch processing with EC50 of 5 nM in the Notch cell-based reporter assay. The potency of RO4929097 in cell-free and cellular assays is in the low nanomolar range with >100-fold selectivity observed with respect to 75 other proteins of various types including receptors, ion channels, and enzymes (CEREP panel). After 5 days of treatment, RO4929097 reduces the production of ICN in the human NSCLC A549 cells inducing a flattened and less transformed tumor cell phenotype in tissue culture [1]. RO4929097 blocks Notch processing in human non-small cell lung carcinoma cells and decreases expression of the Notch transcriptional target gene Hes1. Treatment with RO4929097 reveals a two- to threefold decrease in the expression of direct Notch target genes, Hes1, Hey1, and Heyl in SUM149 and a 3.5- to eightfold decrease in expression in SUM190 cells. RO4929097 modestly inhibits the growth of SUM149 cells in a dose-dependent manner. At a concentration of 1 μM of RO4929097, growth inhibition is 20 % for SUM149 and 10 % for SUM190 cells, relative to vehicle-treated controls. RO4929097 decreases the production of inflammatory cytokines by T-cells. Furthermore, with RO4929097 treatment, there is a shift in favor of TH2 over TH1 cytokines. In addition, T-cell activation induced IL-6 production would be increased with RO4929097 [2]. Upon RO4929097 treatment, the selected melanoma cell lines reveals downregulation of NOTCH downstream effector HES1. A decrease in the amount of melanospheres formed upon RO4929097 treatment in primary melanoma cell lines is detected [3].
in vivo: Oral injection of 3 to 60 mg/kg RO4929097 once daily or twice daily to nude mice bearing A549 NSCLC xenografts for either 7, 14, or 21 days of a 21-day schedule results in significant tumor growth inhibition compared with vehicle-treated animals. The tumor growth inhibition values ranges from 66% to 91%. When mice are treated with 60 mg/kg RO4929097 twice daily with the 7+/14- schedule, treatment initially arouses regression of established A549 tumors. At the end of the 21-day cycle (day 47), tumor growth prevention is still 91% compared with vehicle control mice. Inhibition of tumor growth remains prolonged and sustained up to 34 days post-treatment (day 67). On day 67, these mice are retreated with the same dose of RO4929097 for a second cycle (7 days) until day 74. Importantly, the antitumor effects are sustained after dosing is completed [1]. RO4929097 leads to reduced expression of genes associated with angiogenesis in A549 xenograft model. In contrast, the RO4929097-resistant H460a xenograft displays little change in expression of these genes, underscoring the in vivo anti-angiogenesis mechanism of action of RO4929097 [2].

Protocol (Extracted from published papers and Only for reference)


Chemical Information

M.Wt 469.4 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C₂₂H₂₀F₅N₃O₃
CAS No 847925-91-1
Solvent & Solubility

DMSO: ≥ 49 mg/mL

Preparing Stock Solutions

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

Clinical Information of RO4929097

Product Name Sponsor Only Condition Start Date End Date Phase Last Change Date
RO4929097 National Cancer Institute Metastatic colorectal cancer 31-DEC-10 Phase 2 22-OCT-13
National Cancer Institute; The Cancer Institute of New Jersey Prostate tumor 31-AUG-10 31-AUG-12 Phase 2 07-MAY-13
National Cancer Institute Stage III melanoma 30-SEP-10 Phase 2 04-FEB-13
University of Colorado at Denver and Health Sciences Center Pancreas tumor 31-OCT-10 Phase 2 06-SEP-13
National Cancer Institute Multiple myeloma 31-DEC-10 31-JUL-12 Phase 2 29-OCT-13
National Cancer Institute Stage IV melanoma 30-SEP-10 Phase 2 04-FEB-13

References on RO4929097

Inhibitor Kit

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