|(R)-2-(3-(3-((2-氯-3-(三氟甲基)苄基)(2,2-二苯乙基)氨基)丁氧基)苯基)乙酸|CsnPharm

CAS No.: 610318-54-2

RGX-104 Catalog No. CSN23678

Synonyms: Abequolixron;SB-742881

RGX104 free acid is an agonist of liver-X nuclear hormone receptor (LXR), it can regulate the immune process by activating the ApoE gene.

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技术信息

生物活性

描述Immunotherapy non-responders often harbor high levels of circulating myeloid-derived suppressor cells (MDSC)—an immunosuppressive innate cell population. Therapeutic liver-X nuclear receptor (LXR) agonism reduced MDSC abundance in murine models and in patients. So it is a target for enhancing efficacy of cancer immunotherapy in patients. RGX104 Free Acid is a potent LXRβ agonist. Oral administration of RGX-104 (100 mg/kg) to animals bearing palpable tumors significantly suppressed the growth of multiple cancer types. Co-administration of RGX-104 (100 mg/kg) and anti-PD-1 therapy in the Lewis lung cancer model was well tolerated and yielded synergistic anti-tumor activity in the absence of adjuvant tumor antigen vaccination. Monocytic-MDSCs (CD14⁺Lin^negHLA-DR^low) also exhibited reduced abundance 2–3 weeks after RGX-104 treatment initiation relative to pre-dose levels in 5 of 6 patients. RGX-104 is currently in an ongoing multicenter dose escalation phase 1 trial in patients with metastatic solid cancers or lymphomas^[1]. PAH/RGX-104@PDM/PTX (a dual-pH-sensitivity conjugated micelle system) exhibits superior tumor accumulation as well as tumor penetration, and suppresses 74.88% in vivo tumor growth. More importantly, PAH/RGX-104@PDM/PTX has significantly alleviated tumor immunosuppression by eliminating MDSCs and increasing cytotoxic T lymphocytes infiltration^[2].
参考文献

[1] Tavazoie MF, Pollack I, Tanqueco R, et al. LXR/ApoE Activation Restricts Innate Immune Suppression in Cancer. Cell. 2018;172(4):825‐840.e18
[2] Wan D, Yang Y, Liu Y, et al. Sequential depletion of myeloid-derived suppressor cells and tumor cells with a dual-pH-sensitive conjugated micelle system for cancer chemoimmunotherapy. J Control Release. 2020;317:43‐56

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.6776 mL
- 8.3881 mL
- 16.7763 mL
- 5 mM
- 0.3355 mL
- 1.6776 mL
- 3.3553 mL
- 10 mM
- 0.1678 mL
- 0.8388 mL
- 1.6776 mL

技术信息

CAS号

610318-54-2

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C34H33ClF3NO3

运输

蓝冰

分子量

596.08

别名

Abequolixron;SB-742881

溶解度

DMSO	490.0 mg/mL (822.0 mM)
Water	insoluble

动物实验配方

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