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RGX-104 free form

  Cat. No.:  DC33586   Featured
Chemical Structure
610318-54-2
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Field of application
RGX-104, also known as SB 742881, is a liver X receptor beta agonist with potential immunomodulating and antineoplastic activities. Upon oral administration, RGX-104 selectively targets and binds to LXRbeta, thereby activating LXRbeta-mediated signaling, leading to the transcription of certain tumor suppressor genes and the downregulation of certain tumor promoter genes. This particularly activates the expression of apolipoprotein E (ApoE), a tumor suppressor protein, in tumor cells and certain immune cells. This activates the innate immune system, resulting in depletion of immunosuppressive myeloid-derived suppressor cells (MDSCs), tumor cells and endothelial cells in the tumor microenvironment. This reverses immune evasion, enhances anti-tumor immune responses and inhibits proliferation of tumor cells.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 610318-54-2
Chemical Name: RGX-104 free form
Synonyms: RGX-104 free form, RGX-104; RGX104; RGX 104; SB742881; SB-742881; SB 742881;
SMILES: O=C(O)CC1=CC=CC(OCC[C@H](N(CC2=CC=CC(C(F)(F)F)=C2Cl)CC(C3=CC=CC=C3)C4=CC=CC=C4)C)=C1
Formula: C34H33ClF3NO3
M.Wt: 596.0872
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [1]. Tavazoie MF, et al. LXR/ApoE Activation Restricts Innate Immune Suppression in Cancer. Cell. 2018 Feb 8;172(4):825-840.e18.
Description: RGX-104 (free base) is an orally bioavailable and potent liver-X nuclear hormone receptor (LXR) agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
Target: LXR[1]
In Vivo: Oral administration of RGX-104 to animals bearing palpable tumors significantly suppresses the growth of multiple cancer types. Strong tumor growth suppression is also observed in animals bearing large tumors. In some instances, RGX-104 treatment causes partial or complete tumor regression. What’s more, it is also found that co-administration of RGX-104 with anti-PD-1 is superior to administration of either RGX-104 or anti-PD-1 alone. Importantly, co-administration of RGX-104 with anti-PD-1 therapy is well tolerated by mice, with no overt signs of toxicity[1].
Cell Assay: Bone marrow cells are cultured with B16F10 melanoma cells and GM-CSF for 6 days. On day 3, RGX-104 (2 μM) is added to the culture. The mean number of Gr-1high CD11b+ cells per 50 mL of culture solution is assessed by flow cytometry on day 6[1].
Animal Administration: Mice[1] B16F10 cancer cells are subcutaneously injected into C57BL/6 mice. Following tumor growth to 5-10 mm3 in volume, mice are fed either control chow, chow supplemented with GW3965 (100 mg/kg), or chow supplemented with RGX-104 (100 mg/kg)[1].
References: [1]. Tavazoie MF, et al. LXR/ApoE Activation Restricts Innate Immune Suppression in Cancer. Cell. 2018 Feb 8;172(4):825-840.e18.
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