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Purity: ≥98%
Abequolixron (formerly known as SB742881; RG104; SB-742881) is a novel potent and orally bioavailable liver-X nuclear hormone receptor-beta (LXR) agonist with potential immunomodulating and anticancer activities. It modulates innate immunity via transcriptional activation of the ApoE gene. 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.
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When given orally to mice with visible tumors, RGX-104 (100 mg/kg daily) effectively suppressed the growth of several cancer types. The combination of RGX-104 and anti-PD-1 was found to be more effective than either drug administered alone. Significantly, mice that received RGX-104 in addition to anti-PD-1 treatment did so with good tolerance and showed no overt damage [1].
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Animal/Disease Models: NOD SCID or RAG mice injected with 1×106 SKOV3 ovarian cancer cells[1].
Doses: 100 mg/kg. Route of Administration: Oral administration daily for about 60 days. Experimental Results: Robustly suppressed tumor growth and progression. |
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| 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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| Molecular Formula |
C34H33CLF3NO3
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| Molecular Weight |
596.09
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| CAS # |
610318-54-2
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| Related CAS # |
RGX-104 hydrochloride;610318-03-1
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| 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
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.17 mg/mL (3.64 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (3.49 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.83 mg/mL (1.39 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6776 mL | 8.3880 mL | 16.7760 mL | |
| 5 mM | 0.3355 mL | 1.6776 mL | 3.3552 mL | |
| 10 mM | 0.1678 mL | 0.8388 mL | 1.6776 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
LXR Agonist Treatment Robustly Suppresses Tumor Growth and Progression across a Broad Set of Mouse and Human Tumors.Cell.2018 Feb 8;172(4):825-840.e18. |
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 LXR Agonism Reduces Tumor-Infiltrating and Systemic Myeloid-Derived Suppressor Cells.Cell.2018 Feb 8;172(4):825-840.e18. |
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