Name: RO4929097
Brand: Adooq Bioscience
SKU: A10802
Availability: InStock
Rating: 5 (1 reviews)

Biological Activity

Target & Activity

Target	Activity	Value
γ secretase (Cell-free assay)		4 nM
γ secretase(ICN) (Cell-free assay)		5 nM
Aβ40 (Cell-free assay)		14 nM

Cellular Effect

Cell Line	Activity	Value	Description	Reference
HEK293	EC50	14 nM	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	Inhibition of gamma secretase mediated Notch1 signaling in HEK293 cells expressing truncated human Notch1 by luciferase reporter gene assay	[PMID: 27045975]

In Vitro Studies

In an endometrial cancer screen, RO-4929097 produced different ATP-based viability profiles across models. Figure 6 shows a lower viability AUC in AN3 CA than in RL95-2. This qualitative comparison does not establish an IC50, apoptosis or Notch target engagement. [1]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Model-dependent viability profiles in an endometrial cancer screen

Cell-based study · Endometrial cancer patient-derived organoids REME9 and REME16, compared with AN3 CA and RL95-2 cell lines in the 384-well compound screen [1]

RO-4929097 was included in a 61-agent ATP-based viability screen. Its plotted viability area under the curve was lower in AN3 CA than in RL95-2. The comparison is qualitative; exact AUC values and RO-4929097 IC50 values are not provided by the adopted evidence. The assay does not by itself establish Notch target engagement or apoptosis.

Measured endpoints — not treatment concentrations
Endpoint	Reported result	Reference
ATP-based viability dose-response area under the curve	Viability AUC (qualitative comparison) AN3 CA lower than RL95-2; Figure 6 presents means of triplicate experiments	[1]

Literature-Reported Treatment Conditions

Treatment concentration: Methods: 1.0 nM–20 µM (ten serial dilutions); Figure 6 caption: 0.1–20 µM. The lower bounds conflict.
Exposure duration: 144 h after treatment; compound added 24 h after seeding
Method: 384-well ATP-based viability screen
Vehicle: DMSO; shared assay methods specify maximum 0.1% and vehicle-normalized viability
Reported limits: No RO-4929097-specific numeric AUC table or IC50 in selected evidence. Lower tested concentration differs between Methods and Figure 6 caption; no concentration-specific result adopted.

Methods and source locations

Compound reported in the paper: RO4929097; Compound label in the paper: RO-4929097

Named-compound cellular research only. Supplier attribution belongs to the historical experiment and does not establish current A10802 lot performance.

Table II, RO-4929097 row; Materials and methods, Growth inhibition assays using multi-well plates; Figure 6, RO-4929097 row and caption; Table III

ATP-based viability dose-response area under the curve: CellTiter-Glo 3D viability assay; ATP normalized to vehicle with background subtracted; AUC calculated with Morphit 5.0. No values digitized from bars. — Figure 6, RO-4929097 row and caption; Growth inhibition assays using multi-well plates

In Vivo Studies

In the Pediatric Preclinical Testing Program, RO4929097 at 10 mg/kg/day by oral gavage for a planned 21 days showed limited single-agent activity. EFS differed significantly from controls in 6 of 26 evaluable solid tumor models and none of eight ALL models; no objective responses were reported. Rh10 was excluded because control tumors grew poorly, and the exploratory P values were not adjusted for multiple comparisons. [2]

Limited single-agent activity in pediatric tumor xenografts

Animal study · Pediatric Preclinical Testing Program: 34 mouse xenograft models tested; 26 solid tumor and 8 ALL models evaluable for EFS comparisons [2]

RO4929097 produced statistically significant EFS differences in a subset of solid tumor models, but no objective responses were reported and all evaluable models were classified as low EFS activity. Rh10 was not evaluable because control tumors grew poorly. Significance tests were exploratory and were not adjusted for multiple comparisons.

Measured endpoints — not treatment concentrations
Endpoint	Reported result	Reference
Models with significant event-free survival distribution differences from control	Model count 6/26 (23%) evaluable solid tumor models; 0/8 (0%) evaluable ALL models	[2]
Objective responses and EFS activity classification	Reported response category No PR, CR or MCR reported; no evaluable model met intermediate EFS activity criteria	[2]

Conditions shared by the study groups

Route: Oral gavage
Frequency: Daily
Treatment course: Planned treatment duration 21 days
Vehicle: 1.0% Klucel in water with 0.2% Tween 80

Study groups and reported outcomes
Group / dose	Comparator	Observed result	Reference
RO4929097 single agent across pediatric xenograft panel 10 mg/kg/day	Concurrent control groups, ten mice for solid tumors or eight for ALL per group; exact control dosing formulation not specified in acquired main text	Significant EFS differences in 6/26 solid tumor and 0/8 ALL models, with low EFS activity and no objective responses. Rh10 excluded for poor control growth.	[2]

RO4929097 single agent across pediatric xenograft panel: Model: Female immunodeficient mice; CB17SC-M scid for non-glioma solid tumors, BALB/c nu/nu for glioma and NOD/scid for ALL; Reported limits: Supplement per-mouse accounting/response definitions not retrieved; no direct target-engagement measurement reported in acquired panel results.

Methods and source locations

Compound reported in the paper: RO4929097; Compound label in the paper: RO4929097

Preclinical single-agent observations under this mouse regimen; no clinical efficacy or Adooq lot equivalence inferred.

Materials and Methods, In vivo tumor growth inhibition studies / Statistical Methods / Drugs and Formulation; Results paragraphs 1–2; Table I and footnotes

Models with significant event-free survival distribution differences from control: Exact log-rank test; two-sided P values, unadjusted for multiple comparisons. Ten mice per solid tumor control/treatment group and eight per ALL group were specified. — Results paragraph 2; Table I; Statistical Methods; In vivo tumor growth inhibition studies

Objective responses and EFS activity classification: Authors report objective response categories directly; Table I classifies evaluable models as Low. Supplement definitions were not retrieved, so no categories were independently re-derived. — Results paragraph 2; Table I, Median Group Response and EFS Activity columns

RO4929097 single agent across pediatric xenograft panel · Materials and Methods, In vivo tumor growth inhibition studies / Statistical Methods / Drugs and Formulation; Results paragraphs 1–2; Table I and footnotes

Specifications

Manufacturer	Adooq Bioscience
Actions	Inhibitor
CAS Number	847925-91-1
Applications	Gamma-secretase inhibitor
Formula	C₂₂H₂₀F₅N₃O₃
Molecular Weight	469.4
SMILES	CC(C)(C(=O)NCC(C(F)(F)F)(F)F)C(=O)N[C@H]1C2=CC=CC=C2C3=CC=CC=C3NC1=O

Storage & Solubility

In Vitro Solubility

Reported Solubility

Solvent	Reported Solubility
DMSO	92 mg/mL (195.99 mM)
Water	Insoluble
Ethanol	16 mg/mL

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

In Vivo Preparation

Concentration: 9 mg/mL
Vehicle: 2% DMSO+30% PEG 300+5% Tween+ddH2O

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

[1] Tamura H, Higa A, Hoshi H, et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues. Oncology reports (2018). PMID: 29917168 DOI: 10.3892/or.2018.6501 Source material
[2] Kolb EA, Gorlick R, Keir ST, et al. Initial testing (stage 1) by the pediatric preclinical testing program of RO4929097, a γ-secretase inhibitor targeting notch signaling. Pediatric blood & cancer (2012). PMID: 22052798 DOI: 10.1002/pbc.23290 Source material

Publications

1 publication citing this product

Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168

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RO4929097

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RO4929097 1 mg

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