| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Anticancer agent 310 (compound A9) (0.016-10 μM; 72 h) effectively inhibited the proliferation of various human and mouse tumor cell lines in vitro [1]. Anticancer agent 310 (1.6-40 nM; 12-14 days) inhibited the long-term colony formation ability of HGC27 and AGS gastric cancer cells in a concentration-dependent manner [1]. Anticancer agent 310 (50-100 μM; 2 h) induced the release of nitric oxide from HGC27 and AGS gastric cancer cells [1]. Anticancer agent 310 (2 μM; 12 h) induced mitochondrial reactive oxygen species bursts in HGC27 and AGS gastric cancer cells [1]. Anticancer agent 310 (2 μM) induced mitochondrial membrane potential depolarization in HGC27 and AGS gastric cancer cells, and ROS scavenging reversed this effect [1]. Anticancer agent 310 (2 μM; 36 h) induced apoptosis in HGC27 and AGS gastric cancer cells [1]. Anticancer drug 310 (0.5-2 μM; 24 h) can activate the Bax/Bcl-2-Cyt c-Caspase-9/Caspase-3 mitochondrial apoptosis pathway in HGC27 and AGS gastric cancer cells in an in vitro dose-dependent manner [1]. Anticancer drug 310 (0.5-2 μM; 24 h) downregulates the expression of key enzymes SHMT2 and MTHFD2 in the folate one-carbon metabolism pathway in HGC27 and AGS gastric cancer cells in a dose-dependent manner by inhibiting the transcription factor ATF4 [1]. Anticancer drug 310 (2 μM; 12 h) disrupts the redox homeostasis of HGC27 and AGS gastric cancer cells and reduces the ratios of NADPH/NADP+ and GSH/GSSG [1].
|
|---|---|
| ln Vivo |
Anticancer agent 310 (5-15 mg/kg; intratumoral injection; once daily for 14 days) showed dose-dependent anti-gastric cancer activity in NCG mice [1].
|
| Cell Assay |
Cell viability assay [1]
Cell Types: MCF-7, HepG2, HCT-116, HGC27, U251, AGS, ES-2, A2780, K562, MEG01, CT26 Tested Concentrations: 0.016, 0.08, 0.4, 2, 5, 10 μM Incubation Duration: 72 hours Experimental Results: All tested cell lines showed sub-micromolar inhibitory activity, with IC50 values as follows: MCF-7: 0.19 μM; HepG2: 0.21 μM; HCT-116: 0.22 μM; HGC27: 0.10 μM; U251: 0.14 μM; AGS: 0.02 μM; ES-2: 0.12 μM. μM; A2780: 0.11 μM; K562: 0.12 μM; MEG01: 0.40 μM; CT26: 0.26 μM. Apoptosis analysis [1] Cell Types: HGC27, AGS Tested Concentrations: 2 μM Incubation Duration: 36 hours Experimental Results: The total apoptosis rate of HGC27 cells increased from 10.99% (control group) to 83.1%. The total apoptosis rate of AGS cells was 60.9%. Western Blot Analysis [1] Cell Types: HGC27, AGS Tested Concentrations: 0.5, 1, 2 μM Incubation Duration: 24 hours Experimental Results: In both HGC27 and AGS cells, the expression of cytochrome c, Bax, Cleaved Caspase-9 and Cleaved Caspase-3 in the cytoplasm was upregulated in a dose-dependent manner, while the expression of mitochondrial cytochrome c and Bcl-2 was downregulated. |
| Animal Protocol |
Animal/Disease Models:NCG mice treated with HGC27 tumor fragments [1]
Doses: 5 mg/kg; 10 mg/kg; 15 mg/kg Route of Administration: Intratumoral injection; once daily; 14 days Experimental Results: Tumor weight was reduced in the 5 mg/kg dose group compared to the control group. The tumor growth inhibition rate (TGI) in the 10 mg/kg dose group reached 95.3%, and the tumors of 4 out of 6 mice completely regressed. The TGI in the 15 mg/kg dose group reached 98.78%, and the tumors of 5 out of 6 mice completely regressed. The expression of Ki67, SHMT2, and MTHFD2 in tumor tissues of the 10 mg/kg and 15 mg/kg dose groups was reduced compared to the control group. No significant weight loss or death was observed in any of the dose groups. |
| References |
| Molecular Formula |
C33H36N2O12S
|
|---|---|
| Molecular Weight |
684.71
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C1OCC2=C1CC[C@@]3(C)[C@@]2([H])C[C@H]4[C@]5(O4)[C@@]36[C@@H](O6)[C@H](O7)[C@@]7(C(O)(C)C)[C@H]5OC(CCCCOC8=NON=C8S(=O)(C9=CC=CC=C9)=O)=O
|
| 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 | 1.4605 mL | 7.3024 mL | 14.6047 mL | |
| 5 mM | 0.2921 mL | 1.4605 mL | 2.9209 mL | |
| 10 mM | 0.1460 mL | 0.7302 mL | 1.4605 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
