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Nampt-IN-5 is a novel and potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitor with anticancer activity. It inhibits CYP3A4 activity and has cellular IC50s of 0.7 nM and 3.9 nM against A2780 and COR-L23, respectively.
| ln Vitro |
The cellular IC50s of Nampt-IN-5 (Compound 27) (0-10 nM; 3 days) against A2780 and COR-L23 are 0.7 nM and 3.9 nM, respectively [1]. CYP3A4 inhibition value (0.75 μM), mouse microsomal clearance (110 μl/min·mg), Sol6.8: 0.056 mM, and MDCK Pap AB: 18.6[1] were among the good ADME results displayed by Nampt-IN-5.
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| ln Vivo |
In comparison to vehicle, Nampt-IN-5 (5-30 mg/kg) delivered orally twice daily for 4 days significantly reduces body weight in nude mice [1]. In mice, T1/2 (2.1 h), Cmax (29112 nM), and AUC (61984 nM·h) are demonstrated by Nampt-IN-5 (10 mg/kg; oral) [1].
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| References |
| Molecular Formula |
C25H25N5O2
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|---|---|
| Molecular Weight |
427.4983
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| Exact Mass |
427.2
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| CAS # |
2380013-17-0
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| PubChem CID |
146014464
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| Appearance |
White to off-white solid powder
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| LogP |
3.3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
32
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| Complexity |
620
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(N([H])C1C([H])=C([H])C(=C([H])C=1[H])C([H])([H])N1C(=NC2=C([H])C([H])=C([H])C([H])=C12)OC([H])([H])C([H])([H])[H])N1C([H])([H])C([H])(C2=C([H])N=C([H])C([H])=C2[H])C1([H])[H]
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| InChi Key |
JWEBCHOGBDMGBY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H25N5O2/c1-2-32-25-28-22-7-3-4-8-23(22)30(25)15-18-9-11-21(12-10-18)27-24(31)29-16-20(17-29)19-6-5-13-26-14-19/h3-14,20H,2,15-17H2,1H3,(H,27,31)
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| Chemical Name |
N-[4-[(2-ethoxybenzimidazol-1-yl)methyl]phenyl]-3-pyridin-3-ylazetidine-1-carboxamide
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| Synonyms |
NamptIN5 Nampt IN 5
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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 : ~50 mg/mL (~116.96 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.85 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 25.0 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: ≥ 2.5 mg/mL (5.85 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 25.0 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 | 2.3392 mL | 11.6959 mL | 23.3918 mL | |
| 5 mM | 0.4678 mL | 2.3392 mL | 4.6784 mL | |
| 10 mM | 0.2339 mL | 1.1696 mL | 2.3392 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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