| Size | Price | Stock | Qty |
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| 1mg |
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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 |
KD: 3.58 μM (Nur77) [1].
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| ln Vitro |
Nur77 modulator 1 (10g, 0–20 μM) exhibits less cytotoxicity against LO2 cells (a human normal liver cell line) and strong, broad-spectrum antiproliferative action against all three examined hepatoma cell lines (HepG2, QGY–7703, and SMMC-7721)[1]. In a dose-dependent manner, Nur77 modulator 1 (10g) has the potential to specifically up-regulate Nur77 expression[1]. Nur77-dependent apoptosis is induced by Nur77 modulator 1 (10g, 2.0 μM)[1]. In a dose-dependent manner, Nur77 modulator 1 (10g, 2.0 μM) raised the levels of LC3-II and Beclin1 protein. However, 10g administration did not improve p62 degradation, suggesting that the autophagy produced by 10g is not fully completed [1].
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| ln Vivo |
In a mouse hepatoma HepG2 xenograft, Nur77 modulator 1 (10g, 10 and 20 mg/kg/day) shows strong anti-tumor effect with good tolerability[1].
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| Cell Assay |
Cell Viability Assay[1].
Cell Types: Liver cancer cell lines (HepG2, QGY-7703, and SMMC-7721). Tested Concentrations: 0-20 μM. Incubation Duration: 12-24 hrs (hours). Experimental Results: demonstrated IC50 values of 0.6 µM, 0.89 µM, 1.40 µM and >20 µM in HepG2, QGY-7703, SMMC-7721 and LO2 cells, respectively. decreased the viability in a time -dependent manner. Induced cell morphology alteration, such as cell shrinkage, vesicles accumulated, and decreased cell number. |
| Animal Protocol |
Animal/Disease Models: Nude mouse hepatoma HepG2 xenograft[1].
Doses: 10 and 20 mg/kg/day. Route of Administration: IP, once every day for 15 days. Experimental Results: Lead to substantial suppression of tumor growth. The tumor growth inhibition (TGI ) values at doses of 10mg/kg/day and 20 mg/kg/day were 36.74 % and 62.38 %, respectively. demonstrated almost no influence on the body weight of experimental mice. |
| References |
[1]. Baicun Li, et al. Design, synthesis, and biological evaluation of 5-((8-methoxy-2-methylquinolin-4-yl)amino)-1H-indole-2-carbohydrazide derivatives as novel Nur77 modulators. Eur J Med Chem. 2020 Oct 15;204:112608.
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| Molecular Formula |
C28H25N5O2S
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|---|---|
| Molecular Weight |
495.60
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| CAS # |
2469975-55-9
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
C1(/C=N/NC(=O)C2=CC3C=C(NC4=CC(C)=NC5C4=CC=CC=5OC)C=CC=3N2)C=CC(=CC=1)SC
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : 125 mg/mL (252.22 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (4.20 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.20 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0178 mL | 10.0888 mL | 20.1776 mL | |
| 5 mM | 0.4036 mL | 2.0178 mL | 4.0355 mL | |
| 10 mM | 0.2018 mL | 1.0089 mL | 2.0178 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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