RGX-104 hydrochloride is a small-molecule LXR (liver X receptor) agonist that modulates innate immunity via transcriptional activation of the ApoE gene. Oral administration of RGX-104 hydrochloride to animals bearing palpable tumors significantly suppresses the growth of multiple cancer types. Responses are seen across a wide spectrum of malignancies, including lung cancer, melanoma, glioblastoma, and ovarian, renal cell, triple-negative breast, and colon cancer.
|Solubility (25°C)||DMSO ≥ 70 mg/mL (May need warming)|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
 Masoud F Tavazoie, et al. Cell . LXR/ApoE Activation Restricts Innate Immune Suppression in Cancer
|Related Liver X Receptor Products|
BMS-779788 is a LXR partial agonist with IC50 values of 68 nM for LXRα and 14 nM for LXRβ.
Iristectorigenin B is a liver X receptor (LXR) modulator, which stimulates the transcriptional activity of both LXR-α and LXR-β.
RGX-104, also known as SB 742881, is a liver X receptor beta (LXR) agonist with potential immunomodulating and antineoplastic activities.
Yamogenin (Diosgenin) antagonizes the activation of the liver X receptor (LXR) in luciferase ligand assay.
SR9238 is a liver X receptor (LXR) inverse agonist with IC50s of 214 nM and 43 nM for LXRα and LXRβ, respectively.
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