| Size | Price | |
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| 100mg | ||
| 250mg | ||
| 500mg |
| ln Vitro |
NAMPT/IDO1-IN-1 (Compound 10e) (10 μM; 48 h) is dependent on NAMPT and IDO1 and has antiproliferative effect on A549/R cells[1]. Inhibiting A549/R cell colony formation in a dose-dependent manner, NAMPT/IDO1-IN-1 (5 μM, 10 μM; 24 h) works in tandem with NAMPT and μM, 15 μM; 12 d) to increase intracellular ROS buildup [1]. in A549/R cells decreases NAD+ in a way that is dependent on IDO1[1].
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| ln Vivo |
NAMPT/IDO1-IN-1 (compound 10e) (5 μM; 24 h) has a promoting effect on ROS in zebrafish cells, and its ROS level is considerably lower than LPS (50 μg/mL) treatment [1]. IN-1 (25 mg/kg; IV; single dosage) has good oral bioavailability and (5 mg/kg; IV; single dose) yields moderate overall exposure [1]. IN-1 (50, 100, 200 mg/kg; bucally; twice daily for 3 weeks) has also exhibited in vivo anti-tumor activities in the A549/R tumor xenograft model [1].
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| Animal Protocol |
Animal/Disease Models: Female nude 6-8 week old mice with A549/R cells [1]
Doses: 50, 100 and 200 mg/kg Route of Administration: po (oral gavage); twice (two times) daily for 3 weeks Experimental Results: vs. Compared with single agent, it demonstrated better inhibitory activity against A549/R xenografts. The combination of FK866 and epacadostat demonstrated comparable anti-tumor efficacy at the 100 mg/kg dose, and demonstrated better efficacy than the combination group at the 200 mg/kg dose. |
| References |
[1]. Wang K, et al. Dual Nicotinamide Phosphoribosyltransferase (NAMPT) and Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors for the Treatment of Drug-Resistant Nonsmall-Cell Lung Cancer. J Med Chem. 2023 Jan 12;66(1):1027-1047.
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| Molecular Formula |
C23H24BRFN8O3
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|---|---|
| Molecular Weight |
559.39
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| CAS # |
2247884-06-4
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| SMILES |
C(/C1=NON=C1NCCCCCCNC(C1C=CC2=NC=CN2C=1)=O)(=N\O)\NC1C=CC(=C(C=1)Br)F
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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 | 1.7877 mL | 8.9383 mL | 17.8766 mL | |
| 5 mM | 0.3575 mL | 1.7877 mL | 3.5753 mL | |
| 10 mM | 0.1788 mL | 0.8938 mL | 1.7877 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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