| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
SG-55 (0.5-100 μM; 72 h) did not inhibit the growth of PC-9/OR cell lines (PC-9 EGFR 19Del/T790M/C797S cells) overexpressing AKR1C3 [1]. SG-55 (72 h) reduced the IC50 value of osimertinib (100-500 nM) in PC-9/OR cells from 2.59 μM to 1.30 μM, 0.43 μM and 0.23 μM at concentrations of 10 μM, 20 μM and 50 μM, respectively, with corresponding resistance reversal folds of 2, 6 and 11 times [1]. SG-55 (10 μM) synergistically with osimertinib inhibited colony formation (14 days), reduced cell migration (24 hours), enhanced cell cycle arrest (24 hours) and apoptosis (72 hours), thereby significantly improving the sensitivity of PC-9/OR cells[1]. SG-55 (10 μM; 72 hours)-mediated AKR1C3 inhibition can increase the NADPH/NADP+ ratio, disrupt the GSH cycle, break the redox balance and exacerbate oxidative damage, thereby overcoming osimertinib resistance caused by EGFR mutations in PC-9/OR cells[1].
|
|---|---|
| ln Vivo |
SG-55 (10 mg/kg; orally; once daily for 21 days) significantly increased the density of osimertinib-resistant EGFR C797S tumors in mice[1].
|
| Cell Assay |
Apoptosis analysis [1]
Cell Types: PC-9/OR cell line overexpressing AKR1C3 Tested Concentrations: 10 μM plus osimertinib (100 nM) Incubation Duration: 72 hours Experimental Results: AKR1C3 inhibition enhanced osimertinib-induced apoptosis. Cell cycle analysis [1] Cell Types: AKR1C3 overexpressing PC-9/OR cell line Tested Concentrations: 10 μM plus osimertinib (100 nM) Incubation Duration: 24 hours Experimental Results: Osimertinib alone can cause G0/G1 phase arrest, while the addition of this compound causes the cell cycle distribution to accumulate and shift to the G2/M phase. |
| Animal Protocol |
Animal/Disease Models:3 × 10⁷ PC-9/OR cells (100 μL) were subcutaneously seeded into the right abdomen of 6-week-old male BALB/c nude mice to establish a xenograft tumor model [1].
Doses: 10 mg/kg combined with osimertinib (5 mg/kg, orally). Route of Administration: Oral administration; once daily for 21 days. Experimental Results: Tumor growth inhibition rate (TGI) was 15.6%. When combined with osimertinib, the TGI was 93.1%. No significant weight loss was observed. |
| References |
| Molecular Formula |
C19H17N3O2
|
|---|---|
| Molecular Weight |
319.36
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
N#CC1=CC2=C(C=C1)CN(C(C3=CC(C(C4CC4)=O)=CN3)=O)CC2
|
| 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) |
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
|
|---|---|
| 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 | 3.1313 mL | 15.6563 mL | 31.3126 mL | |
| 5 mM | 0.6263 mL | 3.1313 mL | 6.2625 mL | |
| 10 mM | 0.3131 mL | 1.5656 mL | 3.1313 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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