RGX-104
- SB 742881
Axon 3739
CAS:
610318-54-2
- Optical Purity: 99% e.e.
- Soluble in DMSO
- MF: C34H33ClF3NO3
- MW: 596.08
Description
RGX-104 is an oral, selective LXR (Liver-X Nuclear Hormone Receptor) agonist, and a first-in-class immunotherapy agent. It activates the expression of the ApoE gene and reverses the immunosuppressive effects of cancer by targeting the LXR/ApoE pathway that regulates the innate immune response to cancer. This next-generation therapy has two key effects on the innate immune system that drive tumor immunity: it depletes myeloid-derived suppressor cells (MDSCs) and stimulates dendritic cells (DCs). MDSCs block the ability of T cells to become active, while stimulated DCs are required for proper activation (priming) of T cells.
More Information
| Parent CAS No. | 610318-54-2 |
|---|---|
| Chemical Name | (R)-2-(3-(3-((2-chloro-3-(trifluoromethyl)benzyl)(2,2-diphenylethyl)amino)butoxy)phenyl)acetic acid |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C1C=C(C(C2C=CC=CC=2)CN(CC2C(Cl)=C(C(F)(F)F)C=CC=2)[C@@H](CCOC2C=C(CC(=O)O)C=CC=2)C)C=CC=1 |&1:24,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C34H33ClF3NO3/c1-24(18-19-42-29-16-8-10-25(20-29)21-32(40)41)39(22-28-15-9-17-31(33(28)35)34(36,37)38)23-30(26-11-4-2-5-12-26)27-13-6-3-7-14-27/h2-17,20,24,30H,18-19,21-23H2,1H3,(H,40,41)/t24-/m1/s1 |
| InChiKey | ZLJZDYOBXVOTSA-XMMPIXPASA-N |
| CID | 10218693 |
| Short Description | LXR agonist |
References
- MF Tavazoie et al. LXR/ApoE Activation Restricts Innate Immune Suppression in Cancer. Cell. 2018, 172, 825-840.
- Pharmacodynamic and clinical activity of RGX-104, a first-in-class immunotherapy targeting the liver-X nuclear hormone receptor (LXR), in patients with refractory malignancies. J. Clin Oncol 36, no. 15_suppl (2018) 3095-3095.
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