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Linrodostat mesylate (formerly known as BMS-986205 mesylate, ONO-7701 mesylate and F001287 mesylate) 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).
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| References |
:AACR; Cancer Res. 2017; 77 (13 Suppl): Abstract nr CT116.;Cancer Discov.2018 Jan;8(1):OF3.
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| Molecular Formula |
C25H28CLFN2O4S
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|---|---|
| Molecular Weight |
507.0174
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| Exact Mass |
N/A
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| CAS # |
2221034-29-1
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| Related CAS # |
1923833-60-6;2221034-29-1 (mesylate)
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| SMILES |
C[C@H]([C@H]1CC[C@@H](C2=CC=NC3=CC=C(F)C=C23)CC1)C(NC4=CC=C(Cl)C=C4)=O.CS(=O)(O)=O
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| InChi Key |
LZNFBNWGSDOVIO-QEFLZESTSA-N
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| InChi Code |
InChI=1S/C24H24ClFN2O.CH4O3S/c1-15(24(29)28-20-9-6-18(25)7-10-20)16-2-4-17(5-3-16)21-12-13-27-23-11-8-19(26)14-22(21)231-5(2,3)4/h6-17H,2-5H2,1H3,(H,28,29)1H3,(H,2,3,4)/t15-,16-,17+/m1./s1
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| Chemical Name |
(R)-N-(4-chlorophenyl)-2-((1s,4S)-4-(6-fluoroquinolin-4-yl)cyclohexyl)propanamide methanesulfonic acid
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| Synonyms |
Linrodostat mesylate BMS-986205 BMS 986205 BMS986205 ONO-7701 ONO 7701 ONO7701 F-001287 F001287 F001287 Linrodostat
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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 Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9723 mL | 9.8615 mL | 19.7231 mL | |
| 5 mM | 0.3945 mL | 1.9723 mL | 3.9446 mL | |
| 10 mM | 0.1972 mL | 0.9862 mL | 1.9723 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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