Linrodostat
Linrodostat (CAS 1923833-60-6) is a selective and irreversible inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1). It exhibits potent inhibitory activity against IDO1, with an IC50 value of 1.7 nM, and an IC50 of 1.1 nM in HEK293 cells expressing human IDO1. In contrast, it shows weak inhibitory activity against HEK293 cells expressing TDO (IC50 > 2000 nM), demonstrating high selectivity. Its mechanism of action involves the irreversible inhibition of IDO1, thereby reducing kynurenine production. This compound has shown favorable pharmacological activity and properties in advanced cancer, making it an important tool for related cancer research.
Reference:
[1]. Lillian L. Siu, Karen Gelmon, Quincy Chu, Russell Pachynski, Olatunji Alese, Paul Basciano, Justine Walker, Priyam Mitra, Li Zhu, Penny Phillips, John Hunt, Jayesh Desai; Abstract CT116: BMS-986205, an optimized indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor, is well tolerated with potent pharmacodynamic (PD) activity, alone and in combination with nivolumab (nivo) in advanced cancers in a phase 1/2a trial. Cancer Res 1 July 2017; 77 (13_Supplement): CT116. https://doi.org/10.1158/1538-7445.AM2017-CT116
[2]. From Bench to Bedside. Cancer Res. 2017 Dec 15;77(24):6795-6811. doi: 10.1158/0008-5472.CAN-17-2285. PMID: 29247038; PMCID: PMC6021761.
| Storage | Store at -20°C |
| M.Wt | 410.92 |
| Cas No. | 1923833-60-6 |
| Formula | C24H24ClFN2O |
| Synonyms | BMS-986205; ONO-7701 |
| Solubility | Soluble in DMSO |
| Chemical Name | (R)-N-(4-chlorophenyl)-2-((1s,4S)-4-(6-fluoroquinolin-4-yl)cyclohexyl)propanamide |
| SDF | Download SDF |
| Canonical SMILES | O=C(NC1=CC=C(Cl)C=C1)[C@H](C)[C@@]2([H])CC[C@H](CC2)C3=CC=NC4=C3C=C(F)C=C4 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |