| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
The primary target of NSC756093 is the protein-protein interaction between guanylate binding protein 1 (GBP1) and Pim-1, a serine/threonine kinase. It acts as a potent inhibitor of this interaction, binding to GBP1-Pim-1 with a Kd of 38 nM. By inhibiting the GBP1-Pim-1 interaction, NSC756093 disrupts signaling pathways that promote cell proliferation and survival.
|
|---|---|
| ln Vitro |
In vitro, NSC756093 is a potent inhibitor of the GBP1-Pim-1 interaction. It binds to GBP1-Pim-1 with a Kd of 38 nM and inhibits the interaction by 65% when used at a concentration of 100 nM. The compound inhibits proliferation of paclitaxel-resistant cancer cells. Its activity is typically measured using surface plasmon resonance (SPR) or other biophysical techniques that assess protein-protein interactions. Cell-based assays that measure proliferation, migration, cell cycle, and apoptosis are employed to confirm the compound's biological activity.
|
| ln Vivo |
In vivo, NSC756093 can potentially revert resistance to paclitaxel. It may be used in ovarian cancer research. While specific in vivo efficacy data for NSC756093 are not extensively detailed in the available literature, its mechanism of action suggests that it would be effective in reducing tumor growth and overcoming drug resistance.
|
| Enzyme Assay |
In vitro enzyme/receptor binding assays for NSC756093 involve biophysical techniques such as surface plasmon resonance (SPR) to measure the binding affinity between GBP1 and Pim-1 in the presence of the compound. The compound's ability to inhibit the GBP1-Pim-1 interaction is quantified by measuring the reduction in binding signal. IC50 values are determined from dose-response curves.
|
| Cell Assay |
In vitro cellular assays for NSC756093 are conducted in cancer cell lines, particularly ovarian cancer cells. Cells are treated with varying concentrations of NSC756093, and cell proliferation is measured using MTT, CellTiter-Glo, or colony formation assays. Cell migration is assessed using wound healing or Transwell assays. Cell cycle analysis by flow cytometry and apoptosis assays (caspase activation, annexin V staining) are performed. These assays confirm that NSC756093 engages its target in a cellular context and produces the expected inhibition of cell proliferation, migration, and induction of cell cycle arrest and apoptosis.
|
| Animal Protocol |
In vivo animal studies for NSC756093 would typically be conducted in mouse xenograft models using ovarian cancer cell lines, including paclitaxel-resistant models. Animals would be administered NSC756093 alone or in combination with paclitaxel, and tumor growth inhibition would be monitored. The compound's ability to revert paclitaxel resistance would be assessed. Pharmacokinetic studies would be performed to determine the compound's bioavailability, half-life, and tissue distribution.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of NSC756093 indicate that it has a molecular weight of 337.37 and a molecular formula of C20H19NO4. The compound is a podophyllotoxin analog. 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.
|
| Toxicity/Toxicokinetics |
The toxicological profile of NSC756093 is primarily derived from its use as a research compound in preclinical studies. As an inhibitor of the GBP1-Pim-1 interaction, potential on-target effects could include changes in cell proliferation and survival. Comprehensive toxicology studies would be required for therapeutic development, including assessments of hematopoietic, gastrointestinal, and reproductive function.
|
| Additional Infomation |
NSC756093 is a potent inhibitor of the GBP1-Pim-1 interaction. It binds to GBP1-Pim-1 with a Kd of 38 nM. The compound is a podophyllotoxin analog and inhibits proliferation of paclitaxel-resistant cancer cells. NSC756093 can be used in ovarian cancer research. It is not approved for clinical use and is available from research chemical suppliers for preclinical studies.
|
| Molecular Formula |
C20H19NO4
|
|---|---|
| Molecular Weight |
337.37
|
| Exact Mass |
337.131
|
| CAS # |
1629908-92-4
|
| PubChem CID |
91826517
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.4±0.1 g/cm3
|
| Boiling Point |
561.8±50.0 °C at 760 mmHg
|
| Flash Point |
293.6±30.1 °C
|
| Vapour Pressure |
0.0±1.6 mmHg at 25°C
|
| Index of Refraction |
1.668
|
| LogP |
1.48
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
25
|
| Complexity |
540
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O1C(C2=C(C1([H])[H])N(C([H])([H])C([H])([H])O[H])C1C([H])=C(C([H])=C([H])C=1C2([H])C1C([H])=C([H])C([H])=C([H])C=1[H])OC([H])([H])[H])=O
|
| InChi Key |
SMEJQLRLHKWIFV-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C20H19NO4/c1-24-14-7-8-15-16(11-14)21(9-10-22)17-12-25-20(23)19(17)18(15)13-5-3-2-4-6-13/h2-8,11,18,22H,9-10,12H2,1H3
|
| Chemical Name |
4-(2-hydroxyethyl)-6-methoxy-9-phenyl-3,9-dihydrofuro[3,4-b]quinolin-1-one
|
| Synonyms |
NSC 756093; NSC-756093; NSC756093
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~62.5 mg/mL (~185.26 mM)
|
|---|---|
| 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 | 2.9641 mL | 14.8205 mL | 29.6410 mL | |
| 5 mM | 0.5928 mL | 2.9641 mL | 5.9282 mL | |
| 10 mM | 0.2964 mL | 1.4821 mL | 2.9641 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
