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RGX-104

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Chemical Structure| 610318-54-2 同义名 : Abequolixron
CAS号 : 610318-54-2
货号 : A981571
分子式 : C34H33ClF3NO3
纯度 : 99%+
分子量 : 596.079
MDL号 : MFCD31726291
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(176.15 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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+LinnegHLA-DRlow) 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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.68mL

0.34mL

0.17mL

8.39mL

1.68mL

0.84mL

16.78mL

3.36mL

1.68mL
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