| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
IC50: 5 nM (NAMPT)[1]
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| ln Vitro |
A panel of 53 non-small cell lung cancer (NSCLC) cell lines is used to assess the activity of GNE-617 hydrochloride in the presence or absence of 10 μM nicotinic acid. The majority of cell lines show a high dosage response to GNE-617 as measured by a drop in ATP or total nucleic acid, and the cytotoxicity is entirely restored by the simultaneous injection of nicotinic acid. GNE-617 inhibits NAMPT IC50 of 18.9 nM in A549 cells. About half of the studied cell lines had IC50 values less than 10 nM, while the majority had IC50 values below 100 nM. Nicotinic acid fails to save eighteen cell lines, and those that cannot be saved typically have lower IC50 values (P=0.008, Fisher exact test, IC50<10 nM vs. ≥10 nM)[1].
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| ln Vivo |
In comparison to GMX-1778 (given BID), GNE-617 hydrochloride (administered QD) and GNE-875 (administered BID) in rats are linked to more severe retinal damage at similar doses and dosing durations. The GNE-617, GNE-618, and GMX-1778 mouse efficacy studies are intended to evaluate the product's effectiveness and are opportunistically utilized to evaluate the retinal toxicity in mice. Both GNE-617 and GMX-1778 have been shown to cause NAMPTi retinal toxicity; however, due to their dissimilar research lengths, a direct comparison of their retinal toxicity is not possible[2].
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| References |
[1]. Shames DS, et al. Loss of NAPRT1 Expression by Tumor-specific Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT Inhibitors. Clin Cancer Res. 2013 Dec 15;19(24):6912-23.
[2]. Zabka TS, et al. Retinal toxicity, in vivo and in vitro, associated with inhibition of nicotinamide phosphoribosyltransferase. Toxicol Sci. 2015 Mar;144(1):163-72 |
| Molecular Formula |
C21H16CLF2N3O3S
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|---|---|
| Molecular Weight |
463.88
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| CAS # |
2070014-99-0
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| Related CAS # |
GNE-617;1362154-70-8
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| SMILES |
Cl[H].S(C1C([H])=C(C([H])=C(C=1[H])F)F)(C1C([H])=C([H])C(=C([H])C=1[H])C([H])([H])N([H])C(C1C([H])=C([H])C2=NC([H])=C([H])N2C=1[H])=O)(=O)=O
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| Solubility (In Vitro) |
DMSO: 5.56 mg/mL (11.99 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.56 mg/mL (1.21 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 5.6 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: ≥ 0.56 mg/mL (1.21 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 5.6 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. View More
Solubility in Formulation 3: ≥ 0.56 mg/mL (1.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1557 mL | 10.7786 mL | 21.5573 mL | |
| 5 mM | 0.4311 mL | 2.1557 mL | 4.3115 mL | |
| 10 mM | 0.2156 mL | 1.0779 mL | 2.1557 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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