| Size | Price | Stock | Qty |
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| 100mg |
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| Other Sizes |
| Targets |
BMS-986242 targets indoleamine-2,3-dioxygenase 1 (IDO1). IDO1 is an enzyme that catalyzes the rate-limiting step in the kynurenine pathway of tryptophan metabolism. By depleting tryptophan and producing immunosuppressive kynurenines, IDO1 contributes to the immunosuppressive tumor microenvironment. BMS-986242 is a selective inhibitor of IDO1 with potential antitumor activity.
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| ln Vitro |
BMS-986242 is less susceptible to glucuronidation and more prone to oxidative metabolism. With the exception of nAChR a1 (IC50=12.3 μM) and nAChR a7 (IC50>6 μM, highest inhibitory capability of about 20%), BMS-986242 exhibits IC50>25 μM for all targets [1].
In vitro, BMS-986242 demonstrates potent inhibition of IDO1 enzymatic activity. It shows a higher propensity for oxidative metabolism and reduced susceptibility to glucuronidation. These in vitro characteristics support its use in studying IDO1 biology and for developing cancer immunotherapies. |
| ln Vivo |
BMS-986242 (3 to 30 mg/kg; oral; 0 to 24 hours) revealed dose-proportional exposure and statistically significant decreases in tumor kynurenine concentrations at all three dosages [1 ].
In vivo, BMS-986242 is an orally active IDO1 inhibitor. It has been developed for the treatment of a variety of cancers. Research applications include exploring its use in combination therapies for cancer treatment and investigating its effects on immune response modulation. However, specific published in vivo efficacy studies are not detailed in the current literature. |
| Enzyme Assay |
The in vitro IDO1 inhibition assay for BMS-986242 uses recombinant IDO1 enzyme and a substrate such as L-tryptophan. Enzyme activity is measured by quantifying the production of kynurenine, which can be detected by colorimetric or HPLC methods. The compound is added at various concentrations, and IC50 values are calculated from dose-response curves. Selectivity profiling against other enzymes is performed to confirm specificity.
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| Cell Assay |
Cellular assays for BMS-986242 are conducted in cancer cell lines or immune cells that express IDO1. Cells are treated with varying concentrations of the compound. IDO1 activity is measured by quantifying kynurenine levels in the cell culture supernatant. The compound's effects on T cell proliferation and function are assessed in co-culture assays of cancer cells and T cells. The immunosuppressive tumor microenvironment is evaluated by measuring cytokine levels.
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| Animal Protocol |
Animal/Disease Models: nu/nu (nude) mice[1]
Doses: 3~30 mg/kg Route of Administration: Po Experimental Results: Dose-proportional exposure and statistics of kynurenine concentration in tumors were demonstrated at all three doses Dramatically diminished. In vivo studies for BMS-986242 would typically involve syngeneic mouse models of cancer. The compound is administered orally. Efficacy is assessed by measuring tumor growth inhibition. Immunological parameters such as T cell infiltration, kynurenine levels, and cytokine profiles are evaluated in tumor tissues. Combination studies with immune checkpoint inhibitors may be performed. However, specific published in vivo protocols for BMS-986242 are not available. |
| ADME/Pharmacokinetics |
BMS-986242 is an orally active, potent, and selective IDO1 inhibitor. It has a molecular weight of 410.91 and a molecular formula of C24H24ClFN2O. It demonstrates a higher propensity for oxidative metabolism and reduced susceptibility to glucuronidation. Detailed PK parameters such as half-life and bioavailability are not extensively reported in the provided sources.
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| Toxicity/Toxicokinetics |
Toxicity data for BMS-986242 is not extensively reported in publicly available sources. As with all research compounds, BMS-986242 is intended for research use only and not for human therapeutic applications. Standard in vitro cytotoxicity assays and in vivo tolerability studies would be required for a complete toxicity assessment.
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| References | |
| Additional Infomation |
BMS-986242 (CAS 1923844-48-7) is an orally active, potent, and selective inhibitor of indoleamine-2,3-dioxygenase 1 (IDO1). IDO1 is a critical enzyme in the immunosuppressive tumor microenvironment. By inhibiting IDO1, BMS-986242 has the potential to restore antitumor immunity and is being studied for cancer treatment. It is for research use only.
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| Molecular Formula |
C24H24CLFN2O
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|---|---|
| Molecular Weight |
410.911568641663
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| Exact Mass |
410.16
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| Elemental Analysis |
C, 70.15; H, 5.89; Cl, 8.63; F, 4.62; N, 6.82; O, 3.89
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| CAS # |
1923844-48-7
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| PubChem CID |
121318866
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| Appearance |
White to off-white solid powder
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| LogP |
6.2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
545
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[C@H](C1CCC(CC1)C2=C3C=C(C=CC3=NC=C2)F)NC(=O)C4=CC=C(C=C4)Cl
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| InChi Key |
AOJCHFNHRLPISK-KLAILNCOSA-N
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| InChi Code |
InChI=1S/C24H24ClFN2O/c1-15(28-24(29)18-6-8-19(25)9-7-18)16-2-4-17(5-3-16)21-12-13-27-23-11-10-20(26)14-22(21)23/h6-17H,2-5H2,1H3,(H,28,29)/t15-,16?,17?/m1/s1
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| Chemical Name |
4-chloro-N-[(1R)-1-[4-(6-fluoroquinolin-4-yl)cyclohexyl]ethyl]benzamide
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| Synonyms |
BMS-986242; BMS986242; BMS 986242; linrodostat-analogue;
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| HS Tariff Code |
2934.99.9001
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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 Vitro) |
DMSO : ~250 mg/mL (~608.41 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 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.
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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4336 mL | 12.1681 mL | 24.3362 mL | |
| 5 mM | 0.4867 mL | 2.4336 mL | 4.8672 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.
Link: https://clinicaltrials.gov/ct2/show/NCT03351231
Conditions:CancerProducts are for research use only; We do not sell to patients
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