Omaveloxolone (RTA-408)

Catalog No.S7672 Batch:S767201

Technical Data

Formula	C₃₃H₄₄F₂N₂O₃
Molecular Weight	554.71	CAS No.	1474034-05-3
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (180.27 mM)
		Ethanol	20 mg/mL (36.05 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

Omaveloxolone (RTA-408) is a synthetic triterpenoid that activates the cytoprotective transcription factor Nrf2 and inhibits NF-κB signaling. Phase 2.

Targets

NF-κB ^[1]

Nrf2 ^[1]

In vitro

RTA 408 potently increases expression of Nrf2 target genes and reverses IFNγ-mediated suppression of Gclc expression in RAW 264.7 cells. In a panel of eight human tumor cell lines, RTA 408 inhibits growth with an average GI50 value of 260 nM and induces apoptosis. RTA 408 also inhibits NF-κB and activates JNK in tumor cells. ^[1]

In vivo

In mice with radiation-induced dermatitis, 1.0% RTA 408 markedly reduces epidermal and collagen thickening, prevents dermal necrosis and completely alleviates skin ulcers. ^[2] In rat skin, RTA 408 activates Nrf2 and induces cytoprotective genes. ^[3] RTA 408 also mitigates hematopoietic acute radiation syndrome in mice. ^[4]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines A375, NCI-H460, A2058, MDA-Mb-231, HCT116, 786-0, A549, and PANC-1 cells Concentrations ~1 μM Incubation Time 72 hours Method For growth inhibition assays, cells are plated in duplicate 96-well culture dishes at 3 x 10³ cells per well. The following day, one plate is treated with RTA 408 and the other is immediately processed for the sulforhodamine B (SRB) assay (time 0). Cells in the RTA 408-treated plate are processed for the SRB assay 72 hours after the start of treatment. Percentage of growth relative to vehicle-treated cells is calculated using: [(Ti-Tz)/(C-Tz)] x 100 where (Tz) is the absorbance value at time zero, (C) is absorbance value from vehicle treated wells after 72 hours, and (Ti) is the absorbance value from wells treated with the drug. Dose-response curves are plotted in GraphPad Prism and GI50 values are calculated
Animal Study:^{^[2]}	Animal Models Mice with radiation-induced dermatitis Dosages 1% in 100 μL vehicle (w/v) Administration Topical application

Cell Assay:^{^[1]}

Cell lines
A375, NCI-H460, A2058, MDA-Mb-231, HCT116, 786-0, A549, and PANC-1 cells
Concentrations
~1 μM
Incubation Time
72 hours
Method
For growth inhibition assays, cells are plated in duplicate 96-well culture dishes at 3 x 10³ cells per well. The following day, one plate is treated with RTA 408 and the other is immediately processed for the sulforhodamine B (SRB) assay (time 0). Cells in the RTA 408-treated plate are processed for the SRB assay 72 hours after the start of treatment. Percentage of growth relative to vehicle-treated cells is calculated using: [(Ti-Tz)/(C-Tz)] x 100 where (Tz) is the absorbance value at time zero, (C) is absorbance value from vehicle treated wells after 72 hours, and (Ti) is the absorbance value from wells treated with the drug. Dose-response curves are plotted in GraphPad Prism and GI50 values are calculated

Animal Study:^{^[2]}

Animal Models
Mice with radiation-induced dermatitis
Dosages
1% in 100 μL vehicle (w/v)
Administration
Topical application

References

[4] Goldman DC, et al. Radiat Res. 2015, 183(3), 338-344.

+ Expand

Selleck's Omaveloxolone (RTA-408) has been cited by 6 publications

Synthetic oleanane triterpenoids suppress MYB oncogene activity and sensitize T-cell acute lymphoblastic leukemia cells to chemotherapy [ Front Oncol, 2023, 13:1126354]	PubMed: 37077825
Neonatal ketone body elevation regulates postnatal heart development by promoting cardiomyocyte mitochondrial maturation and metabolic reprogramming [ Cell Discov, 2022, 8(1):106]	PubMed: 36220812
RTA-408 protects against propofol-induced cognitive impairment in neonatal mice via the activation of Nrf2 and the inhibition of NF-κB p65 nuclear translocation [ Brain Behav, 2021, 11(1):e01918]	PubMed: 33295701
A Human Organoid Model of Aggressive Hepatoblastoma for Disease Modeling and Drug Testing [ Cancers (Basel), 2020, 12(9)E2668]	PubMed: 32962010
Inhibition of Nrf2 might enhance the anti-tumor effect of temozolomide in glioma cells via inhibition of Ras/Raf/MEK signaling pathway. [ Int J Neurosci, 2020, 7:1-16]	PubMed: 32378973
Olean-28,13b-olide 2 plays a role in cisplatin-mediated apoptosis and reverses cisplatin resistance in human lung cancer through multiple signaling pathways. [ Biochem Pharmacol, 2019, 170:113642]	PubMed: 31541631

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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