| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Targets |
RNR ( IC50 = 250 nM ); RNR ( IC50 = 32 μM )
Ribonucleotide reductase (RR), specifically the large subunit (hRRM1) of human RR (hRR). NSAH inhibits RR, which is the rate-limiting enzyme for de novo deoxyribonucleotide synthesis, thereby inhibiting DNA synthesis and cell proliferation. |
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| ln Vitro |
NSAH inhibits RR in cells by lowering the amounts of dGTP and dATP in the dNTP pool, which results in S-phase arrest[1].
NSAH (0-10 μM, 2, 6, 24, or 72 h) demonstrates strong anti-tumor activity in three cancer cell lines[1]. NSAH inhibits the rate and timing of dATP and dGTP decreases, which effectively stops S-phase progression[1]. NSAH inhibits hRR with a cell-free IC50 of 32 µM and a cell-based IC50 of ~250 nM. It exhibits potent cytotoxicity toward cancer cells while demonstrating very moderate toxicity against normal blood progenitor cells. |
| ln Vivo |
Specific in vivo activity data for NSAH are not detailed in the available literature. As an RR inhibitor, it would be expected to have antitumor activity in vivo. However, specific animal model studies are not described.
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| Enzyme Assay |
The in vitro enzyme inhibition assay for NSAH involves measuring the activity of ribonucleotide reductase in the presence of varying concentrations of the compound. The enzyme is incubated with its substrate (CDP or ADP) and reducing equivalents, and the production of deoxynucleotides is quantified. The IC50 is determined from the dose-response curve.
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| Cell Assay |
Cell Line: MDA-231, HCT116 and Panc1 cancer cell lines.
Concentration: 0-10 μM. Incubation Time: 2, 6, 24, or 72 h. Result: Resulted in IC50 values ranging from 220 to 500 nM. Specific in vitro cell-based assay protocols for NSAH are not detailed. Its cytotoxic effects can be assessed in cancer cell lines by treating cells with NSAH and measuring cell viability using standard assays such as MTT or CellTiter-Glo. Its selectivity can be assessed by comparing its effects on cancer cells versus normal cells. |
| Animal Protocol |
Specific in vivo animal model protocols for NSAH are not described. To evaluate its in vivo efficacy, NSAH could be administered to mouse xenograft models of cancer. Tumor growth inhibition would be measured.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for NSAH are not reported in the available literature. As a research compound, its absorption, distribution, metabolism, and excretion (ADME) properties have not been extensively characterized.
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| Toxicity/Toxicokinetics |
NSAH exhibits potent cytotoxicity toward cancer cells while demonstrating very moderate toxicity against normal blood progenitor cells. This suggests a favorable selectivity profile. Specific toxicological data are not otherwise available.
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| References | |
| Additional Infomation |
NSAH is a research tool for studying ribonucleotide reductase function and for investigating the potential of RR as a therapeutic target for cancer. It is a cell-permeable, potent, and selective non-nucleoside reversible inhibitor. It is not an approved therapeutic agent.
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| Molecular Formula |
C18H14N2O3
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|---|---|
| Molecular Weight |
306.315364360809
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| Exact Mass |
306.1
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| Elemental Analysis |
C, 70.58; H, 4.61; N, 9.15; O, 15.67
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| CAS # |
1099592-35-4
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| Related CAS # |
(E/Z)-NSAH;54009-54-0
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| PubChem CID |
135458654
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| Appearance |
Solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.647
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| LogP |
6.08
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
440
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OC1C=CC2C=CC=CC=2C=1/C=N\NC(C1C=CC=CC=1O)=O
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| InChi Key |
ZZSJOLDICPVVAV-YBFXNURJSA-N
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| InChi Code |
InChI=1S/C18H14N2O3/c21-16-8-4-3-7-14(16)18(23)20-19-11-15-13-6-2-1-5-12(13)9-10-17(15)22/h1-11,21-22H,(H,20,23)/b19-11+
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| Chemical Name |
2-hydroxy-N-[(E)-(2-hydroxynaphthalen-1-yl)methylideneamino]benzamide
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| Synonyms |
Naphthyl salicylic acyl hydrazone; NSAH
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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: 61~62.5 mg/mL (199.1~204.0 mM)
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2646 mL | 16.3228 mL | 32.6456 mL | |
| 5 mM | 0.6529 mL | 3.2646 mL | 6.5291 mL | |
| 10 mM | 0.3265 mL | 1.6323 mL | 3.2646 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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