RGX-104 Hydrochloride (Synonyms: Abequolixron hydrochloride) |
| Catalog No.GC19448 |
RGX-104는 ApoE 유전자의 전사 활성화를 통해 선천 면역을 조절하는 소분자 LXR 작용제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 610318-03-1
Sample solution is provided at 25 µL, 10mM.
RGX-104 Hydrochloride is an orally active liver X receptor (LXR) agonist that modulates innate immunity by activating the transcription of the apolipoprotein E (ApoE) gene[1, 2]. Up-regulation of ApoE promotes the clearance of immunosuppressive cells, such as myeloid-derived suppressor cells (MDSCs) and regulatory T cells (Tregs), thereby reversing the immunosuppressive state of the tumor microenvironment and enhancing antitumor immune responses[3]. RGX-104 Hydrochloride also exhibits antitumor activity and induces cell pyroptosis[4, 5].
References:
[1] Tavazoie M F, Pollack I, Tanqueco R, et al. LXR/ApoE activation restricts innate immune suppression in cancer[J]. Cell, 2018, 172(4): 825-840. e18.
[2] Mita M, Mita A, Chmielowski B, et al. Abstract B001: A phase 1 trial of RGX-104, a first-in-class immunotherapy targeting the liver-X nuclear hormone receptor (LXR), in patients with refractory malignancies[J]. Molecular Cancer Therapeutics, 2018, 17(1_Supplement): B001-B001.
[3] Zhang J, Zhu X, Han L, et al. Cholesterol Metabolism-Mediated Immune Regulation and Cancer Immunotherapy[J]. Available at SSRN 4760648.
[4] Liang H, Shen X. LXR activation radiosensitizes non-small cell lung cancer by restricting myeloid-derived suppressor cells[J]. Biochemical and Biophysical Research Communications, 2020, 528(2): 330-335.
[5] Qiu W, Su W, Xu J, et al. Immunomodulatory‐Photodynamic Nanostimulators for Invoking Pyroptosis to Augment Tumor Immunotherapy[J]. Advanced Healthcare Materials, 2022, 11(21): 2201233.
| Cas No. | 610318-03-1 | SDF | |
| Synonyms | Abequolixron hydrochloride | ||
| Canonical 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.Cl | ||
| Formula | C34H34Cl2F3NO3 | M.Wt | 632.54 |
| Solubility | DMSO : ≥ 130 mg/mL (218.09 mM);Water : < 0.1 mg/mL (insoluble) | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.5809 mL | 7.9046 mL | 15.8093 mL |
| 5 mM | 316.2 μL | 1.5809 mL | 3.1619 mL |
| 10 mM | 158.1 μL | 790.5 μL | 1.5809 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)
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