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Purity: ≥98%
Linrodostat (formerly known as BMS-986205, ONO-7701 and F001287) is a novel, potent, orally bioactive and selective inhibitor of IDO (indoleamine 2,3-dioxygenase 1) with potential anticancer activities. It is licensed by Flexus Inc. to Bristol-Myers Squibb for clinical development. This compound appears to act as an irreversible inhibitor of high potency (~2 nmol/L) with superior pharmacokinetics relative to epacadostat and navoximod. In 2015, BMS-986205 entered a phase I/II study in melanoma patients as monotherapy and in combination with nivolumab (NCT02658890). An interim report noted the compound was well tolerated in patients. A second phase I study of the same combination is being conducted in various other types of advanced cancer patients (NCT03192943).
| ln Vitro |
When SKOV-3 and Jurkat clone E6-1 cells are treated with linrodostat (0.01-100 μM) for 72 hours, the proportion of viable cells is lower than when the control group is left untreated. With an IC50 of 6.3 μM, linrodostat likewise causes cell death at substantially lower concentrations[1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: SKOV-3 and Jurkat clone E6-1 cells Tested Concentrations: 0.01-100 μM Incubation Duration: 72 hrs (hours) Experimental Results: decreased the number of viable cells compared with the non-treated control and induced cell death at much lower concentrations. |
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| References |
[1]. Richards T, et al. Cell based functional assays for IDO1 inhibitor screening and characterization. Oncotarget. 2018 Jul 20;9(56):30814-30820.
[2]. Lillian L. Siu, et al. 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. AACR; Cancer Res. 2017; 77 (13 Suppl): Abstract nr CT116. |
| Molecular Formula |
C24H24CLFN2O
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| Molecular Weight |
410.92
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| CAS # |
1923833-60-6
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| Related CAS # |
1923833-60-6;2221034-29-1 (mesylate);1791396-46-7 (dimesylate );
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| SMILES |
O=C(NC1=CC=C(Cl)C=C1)[ C@H](C)[C@@](CC2)([H])CC[ C@H]2C3=CC=NC4=C3C=C(F)C=C4
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.08 mM) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (6.08 mM) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.06 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 2.08 mg/mL (5.06 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 5: ≥ 2.08 mg/mL (5.06 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4336 mL | 12.1678 mL | 24.3356 mL | |
| 5 mM | 0.4867 mL | 2.4336 mL | 4.8671 mL | |
| 10 mM | 0.2434 mL | 1.2168 mL | 2.4336 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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