Linrodostat | IDO1 inhibitor

CAS:
 1923833-60-6
Catalog Number:
 10-4473

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Linrodostat (1923833-60-6) is an irreversible inhibitor (IC50 = 1.1 nM HEK293 cells; 1.7 nM HeLa cells) of indoleamine 2,3-dioxygenase 1 (IDO1), an enzyme that metabolizes tryptophan into immunosuppressive kynurenine.1,2,3  Acts synergistically with PD-1 inhibitors in various cancer models including bladder4, advanced solid tumors5, and hematologic5.

References/Citations:

  1. Pham and Yeh (2018), Mapping the Binding Trajectory of a Suicide Inhibitor in Human Indoleamine 2,3-Dioxygenase 1; J. Am. Chem. Soc. 140 14538
  2. Feng et al. (2020), Development of Indoleamine 2,3-Dioxygenase 1 Inhibitors for Cancer Therapy and Beyond: A Recent Perspective; J. Med. Chem. 63 15115
  3. Balog et al. (2021), Preclinical Characterization of Linrodostat Mesylate, a Novel, Potent, and Selective Oral Indoleamine 2,3-Dioxygenase 1 Inhibitor; Mol. Cancer Ther. 20 467
  4. Sonpavde et al. (2020), ENERGIZE: a Phase III study of neoadjuvant chemotherapy alone or with nivolumab with/without linrodostat mesylate for muscle-invasive bladder cancer; Future Oncol. 16 4359
  5. Luke et al. (2025), Phase ½ Study of the Indoleamine 2,3-Dioxygenase 1 Inhibitor Linrodostat Mesylate Combined with Nivolumab or Nivolumab and Ipilimumab in Advanced Solid Tumors or Hematologic Malignancies; Clin. Cancer Res. 31 2134
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CAS:
1923833-60-6
Catalog Number:
10-4473
Activity:
IDO1 inhibitor
Chemical Names:
(2R)-N-(4-Chlorophenyl)-2-[4-(6-fluoroquinolin-4-yl)cyclohexyl]propenamide
Alternate Name:
BMS-986205
Molecular Weight:
410.92
Molecular Formula:

C24H24ClFN2O

Solubility:
Soluble in DMSO (>75 mg/ml)
Physical Properties:
White solid
Purity:

>98% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

Download Safety Data Sheet

Product Data Sheet:

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Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

Linrodostat (1923833-60-6) is an irreversible inhibitor (IC50 = 1.1 nM HEK293 cells; 1.7 nM HeLa cells) of indoleamine 2,3-dioxygenase 1 (IDO1), an enzyme that metabolizes tryptophan into immunosuppressive kynurenine.1,2,3  Acts synergistically with PD-1 inhibitors in various cancer models including bladder4, advanced solid tumors5, and hematologic5.

References/Citations:

  1. Pham and Yeh (2018), Mapping the Binding Trajectory of a Suicide Inhibitor in Human Indoleamine 2,3-Dioxygenase 1; J. Am. Chem. Soc. 140 14538
  2. Feng et al. (2020), Development of Indoleamine 2,3-Dioxygenase 1 Inhibitors for Cancer Therapy and Beyond: A Recent Perspective; J. Med. Chem. 63 15115
  3. Balog et al. (2021), Preclinical Characterization of Linrodostat Mesylate, a Novel, Potent, and Selective Oral Indoleamine 2,3-Dioxygenase 1 Inhibitor; Mol. Cancer Ther. 20 467
  4. Sonpavde et al. (2020), ENERGIZE: a Phase III study of neoadjuvant chemotherapy alone or with nivolumab with/without linrodostat mesylate for muscle-invasive bladder cancer; Future Oncol. 16 4359
  5. Luke et al. (2025), Phase ½ Study of the Indoleamine 2,3-Dioxygenase 1 Inhibitor Linrodostat Mesylate Combined with Nivolumab or Nivolumab and Ipilimumab in Advanced Solid Tumors or Hematologic Malignancies; Clin. Cancer Res. 31 2134

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