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| 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. |
MSDS
| TITLE | DOWNLOAD |
| MSDS_15897_DC33586_610318-54-2 |
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