| 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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| 250mg |
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| Targets |
The primary target of NSC49652 is the p75 neurotrophin receptor (p75NTR), a death receptor that plays critical roles in neuronal development, survival, and apoptosis. It acts as a functional agonist of p75NTR, targeting the transmembrane domain (TMD) of the receptor. NSC49652 alters the relative conformation of p75NTR TMDs and induces dynamic changes in the full-length receptor in mammalian cells. By activating p75NTR, NSC49652 triggers p75NTR-dependent cancer cell death.
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| ln Vitro |
In vitro, NSC49652 is a functional p75NTR agonist. It targets the transmembrane domain of p75NTR. NSC49652 induces apoptosis and affects the viability of melanoma cells. The compound has an IC50 of 10 μM in AraTM assays. Its activity is typically measured using cell-based assays that assess apoptosis and cell viability in melanoma cell lines.
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| ln Vivo |
In vivo, NSC49652 is orally active. It induces apoptosis and affects the viability of melanoma cells. While specific in vivo efficacy data for NSC49652 are not extensively detailed in the available literature, its mechanism of action and in vitro activity suggest that it would be effective in reducing tumor growth in melanoma models.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for NSC49652 are not conventional enzyme inhibition studies, as the compound is a receptor agonist rather than an enzyme inhibitor. Instead, the primary assays involve binding studies using cell membranes expressing p75NTR. In these assays, NSC49652 is applied to cells, and its ability to induce conformational changes in p75NTR is assessed. Functional assays that measure apoptosis and cell viability are employed to confirm the compound's agonist activity.
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| Cell Assay |
In vitro cellular assays for NSC49652 are conducted in melanoma cell lines. Cells are treated with varying concentrations of NSC49652, and apoptosis is assessed by measuring caspase activation, annexin V staining, or PARP cleavage. Cell viability is measured using MTT or CellTiter-Glo assays. These assays confirm that NSC49652 engages its target in a cellular context and produces the expected induction of apoptosis and reduction of cell viability.
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| Animal Protocol |
In vivo animal studies for NSC49652 would typically be conducted in mouse xenograft models using melanoma cell lines. Animals would be administered the compound orally, and tumor growth inhibition would be monitored. Apoptosis in tumors would be assessed by immunohistochemistry or TUNEL staining. Pharmacokinetic studies would be performed to determine the compound's oral bioavailability, half-life, and tissue distribution.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of NSC49652 indicate that it has a molecular weight of 225.24 and a molecular formula of C13H15NO3. The compound is orally active, enabling convenient administration for in vivo studies. It is soluble in DMSO, facilitating its use in in vitro assays and formulation for in vivo administration. For storage, the powder should be kept under appropriate conditions to maintain stability.
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| Toxicity/Toxicokinetics |
The toxicological profile of NSC49652 is primarily derived from its use as a research compound in preclinical studies. As a p75NTR agonist, potential on-target effects could include changes in neuronal survival and apoptosis, given the role of p75NTR in these processes. Comprehensive toxicology studies would be required for therapeutic development, including assessments of neurological function.
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| Additional Infomation |
NSC49652 is a reversible, orally active agonist of the p75 neurotrophin receptor (p75NTR). It targets the transmembrane domain of p75NTR and induces apoptosis in melanoma cells. NSC49652 is not approved for clinical use and is available from research chemical suppliers for preclinical studies.
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| Molecular Formula |
C14H11NO2
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| Molecular Weight |
225.247
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| Exact Mass |
225.078
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| CAS # |
908563-68-8
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| PubChem CID |
5356048
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
414.3±45.0 °C at 760 mmHg
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| Flash Point |
204.4±28.7 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.661
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| LogP |
2.76
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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 |
3
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| Heavy Atom Count |
17
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| Complexity |
288
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(C1C=CC=CC=1O)(=O)/C=C/C1C=NC=CC=1
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| InChi Key |
CRWNZUBUBIULHB-BQYQJAHWSA-N
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| InChi Code |
InChI=1S/C14H11NO2/c16-13-6-2-1-5-12(13)14(17)8-7-11-4-3-9-15-10-11/h1-10,16H/b8-7+
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| Chemical Name |
(E)-1-(2-hydroxyphenyl)-3-pyridin-3-ylprop-2-en-1-one
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| Synonyms |
NSC 49652; NSC-49652; NSC49652
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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 : ≥ 20.83 mg/mL (~92.48 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 | 4.4395 mL | 22.1976 mL | 44.3951 mL | |
| 5 mM | 0.8879 mL | 4.4395 mL | 8.8790 mL | |
| 10 mM | 0.4440 mL | 2.2198 mL | 4.4395 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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