| 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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| Other Sizes |
| Targets |
SCH-54292 targets the interaction between Ras and guanine nucleotide exchange factors (GEFs). It inhibits GDP exchange, preventing the activation of Ras by blocking the exchange of GDP for GTP. By inhibiting Ras-GEF interaction, SCH-54292 disrupts Ras-mediated signaling pathways that are critical for cell proliferation, survival, and transformation. This mechanism makes it a valuable tool for studying Ras-driven cancers and other diseases.
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| ln Vitro |
In vitro, SCH-54292 has been shown to inhibit Ras-GEF interaction with an IC50 of 0.7 μM. The compound specifically inhibits GDP exchange, preventing Ras activation. This inhibition disrupts downstream Ras signaling pathways, including the RAF-MEK-ERK and PI3K-AKT pathways. SCH-54292 has been used in cell-based assays to demonstrate the importance of Ras-GEF interactions in cancer cell proliferation and survival.
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| ln Vivo |
In vivo, SCH-54292 has been studied in preclinical models of Ras-driven cancers. The compound has shown potential as a therapeutic agent for targeting Ras signaling. However, further in vivo studies are needed to fully evaluate its efficacy and safety. The compound is used in research to validate Ras-GEF interaction as a therapeutic target and to develop more potent analogs.
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| Enzyme Assay |
The in vitro enzyme inhibition assay for SCH-54292 measures its ability to inhibit GDP exchange activity. The assay is performed using purified Ras protein and GEF, with fluorescently labeled or radiolabeled GDP/GTP as substrates. The exchange reaction is monitored by fluorescence polarization, scintillation counting, or other suitable methods. IC50 values are calculated from dose-response curves. Selectivity is assessed by testing the compound against other GEFs or related targets.
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| Cell Assay |
In vitro cellular studies are conducted using cancer cell lines with aberrant Ras signaling. Cells are treated with SCH-54292 at various concentrations (typically μM ranges) for defined time periods. Cell viability is assessed using MTT or CellTiter-Glo assays. Ras activation is measured by pull-down assays for GTP-bound Ras. Downstream signaling (ERK, AKT phosphorylation) is evaluated by Western blot. Cell proliferation and apoptosis are assessed by standard methods.
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| Animal Protocol |
In vivo animal experiments are performed using xenograft models of Ras-driven cancers. Tumor-bearing mice are administered SCH-54292 via intraperitoneal injection or oral gavage at various doses. Tumor volume is measured over time, and endpoints include tumor growth inhibition, survival, and pharmacodynamic markers. Ras activation and downstream signaling are evaluated in tumor tissues by Western blot or immunohistochemistry.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of SCH-54292 include solubility in DMSO. The compound has a molecular weight of 520.55 g/mol, density of 1.6±0.1 g/cm³, boiling point of 810.0±75.0°C at 760 mmHg, and LogP of 3.96. It appears as a solid at room temperature. Storage at -20°C for powder and -80°C for solutions is recommended. The compound should be protected from light and moisture.
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| Toxicity/Toxicokinetics |
Toxicological data for SCH-54292 are limited to preclinical studies. The compound is for research use only and not intended for human therapeutic applications. No significant toxicity has been reported at effective doses in animal studies. Standard safety precautions should be followed when handling the compound due to its potent biological activity. Long-term toxicity and carcinogenicity studies have not been conducted.
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| Additional Infomation |
SCH-54292 is also known as SCH54292, N-Beta-D-Glucopyranosyl-4-(Hydroxyamino)-N-[2-(2-Naphthalenyloxy)Ethyl]-Benzenesulfonamide. It is a potent and highly specific inhibitor of GDP exchange and Ras-GEF interaction with an IC50 of 0.7 μM. The compound is used in cancer research to study Ras signaling pathways. It is supplied as a powder with ≥98% purity and should be stored under recommended conditions.
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| Molecular Formula |
C24H28N2O9S
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|---|---|
| Molecular Weight |
520.5521
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| Exact Mass |
520.151
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| CAS # |
188480-51-5
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| PubChem CID |
16082414
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
810.0±75.0 °C at 760 mmHg
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| Flash Point |
443.7±37.1 °C
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| Vapour Pressure |
0.0±3.0 mmHg at 25°C
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| Index of Refraction |
1.730
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| LogP |
3.96
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
36
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| Complexity |
789
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| Defined Atom Stereocenter Count |
5
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| SMILES |
S(C1C([H])=C([H])C(=C([H])C=1[H])N([H])O[H])(N(C([H])([H])C([H])([H])OC1C([H])=C([H])C2=C([H])C([H])=C([H])C([H])=C2C=1[H])[C@@]1([H])[C@@]([H])([C@]([H])([C@@]([H])([C@@]([H])(C([H])([H])O[H])O1)O[H])O[H])O[H])(=O)=O
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| InChi Key |
KVPUAIYIBNDBLI-GNADVCDUSA-N
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| InChi Code |
InChI=1S/C24H28N2O9S/c27-14-20-21(28)22(29)23(30)24(35-20)26(36(32,33)19-9-6-17(25-31)7-10-19)11-12-34-18-8-5-15-3-1-2-4-16(15)13-18/h1-10,13,20-25,27-31H,11-12,14H2/t20-,21-,22+,23-,24-/m1/s1
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| Chemical Name |
4-(hydroxyamino)-N-(2-naphthalen-2-yloxyethyl)-N-[(2R,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]benzenesulfonamide
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 1.9210 mL | 9.6052 mL | 19.2105 mL | |
| 5 mM | 0.3842 mL | 1.9210 mL | 3.8421 mL | |
| 10 mM | 0.1921 mL | 0.9605 mL | 1.9210 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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