| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
COX-2 Bax Bcl-2
|
|---|---|
| ln Vitro |
In A549 cancer cells, antitumor agent-78 (compound 2b) (30 μM; 4 h) shows good liposoluble and improved cellular uptake[1]. Antitumor agent-78 (20 μM; 36 h) causes cytotoxicity by causing A549 cancer cells to undergo apoptosis [1]. Antitumor agent-78 (20 μM; 24 h) significantly down-regulates Bcl-2 and up-regulates Bax, along with increasing E-cadherin and decreasing vimentin[1]. Cell cycle arrest at S phase and G2/M phase is caused by antitumor agent-78 (20 μM; 24 h)[1]. Cell migration is inhibited by antitumor agent-78 (10 μM; 12 h) at a 53% inhibition rate[1].
|
| ln Vivo |
Antitumor agent-77 (compound 2a) (6 μg/kg; intravenous; administered on days 8, 10, and 12) exhibits more potential antitumor activity than Oxaliplatin, without causing appreciable weight loss or renal or liver damage[1].
|
| Cell Assay |
Apoptosis Analysis[1]
Cell Types: A549 cells Tested Concentrations: 20 μM Incubation Duration: 36 hrs (hours) Experimental Results: Resulte cell apopsotsis with average apoptotic values (including both early and late apoptotic states which were displayed in Q1-LR and Q1-UR, respectively) of 35.86%. Western Blot Analysis[1] Cell Types: A549 cells Tested Concentrations: 20 μM Incubation Duration: 24 hrs (hours) Experimental Results: Elevated the level of cleaved caspase-3 and diminished the level of caspase-3 in A549 cells. diminished anti-apoptotic protein Bcl-2 and increased pro-apoptotic protein Bax. Elevated the expression of E-cadherin and on the other hand, lowered the protein level of Vimentin. Cell Cycle Analysis[1] Cell Types: A549 cells Tested Concentrations: 20 μM Incubation Duration: 24 hrs (hours) Experimental Results: Blocked cell cycle progression in S and G2/M phase with the values of 24.91% and 22.21%, respectively. |
| Animal Protocol |
Animal/Disease Models: A549 xenograft models in mouse[1]
Doses: 6 μg/kg Route of Administration: intravenous (iv) injection; administration on day 8, 10, 12 after establishing xenograft models (A549 cells; sc) Experimental Results: Dramatically repressed tumor growth, and maintained normal kidney and liver architecture in mice. |
| References |
| CAS # |
2870703-23-2
|
|---|---|
| Appearance |
Typically exists as solid at room temperature
|
| 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.) |
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
