| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Antiproliferative agent-23 (72 hours) has anti-proliferative activities against HepG2 (IC50=0.86), MDA-MB-231 (IC50=1.53), MCF-7 (IC50=0.94), A2780 (IC50=0.88), A549 (IC50=0.23), A549/CDDP (IC50=0.35), HepG2/CDDP (IC50=1.16), and HUEVC (IC50=5.68) [1]. A549/CDDP cells can be efficiently induced to undergo apoptosis by antiproliferative agent-23 (5 μM) during a 24-hour period [1]. Antiproliferative agent-23 (5 μM; 24 hours) can efficiently damage DNA in A549/CDDP cells, which in turn causes cell death. The expression of proteins linked to ER stress is markedly upregulated by antiproliferative agent-23 [1]. Polymerization inhibition is caused by antiproliferative agent-23 (10, 20 μM; 24 hours) with an ic50 of 9.86 μM [1]. A549/CDDP cells' intracellular ROS is markedly increased by antiproliferative agent-23 (5 μM; 24 hours)[1]. In vitro tests show that antiproliferative agent-23 (1 μM; 24 hours) efficiently suppresses A549 cell migration [1].
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|---|---|
| ln Vivo |
In order to lessen CDDP resistance, antiproliferative agent-23 (12.40 mg/kg); intravenously; once every 7 days; for 28 days in a row] has antitumor activity and maintains excellent antitumor efficiency [1].
|
| Cell Assay |
Apoptosis Analysis[1]
Cell Types: CDDP-resistant non-small cell lung cancer cell line(A549/CDDP) Tested Concentrations: 5 μM Incubation Duration: 24 hrs (hours) Experimental Results: Effectively induced cell apoptosis in A549/CDDP cells. Western Blot Analysis[1] Cell Types: CDDP-resistant non-small cell lung cancer cell line(A549/CDDP) Tested Concentrations: 5 μM Incubation Duration: 24 hrs (hours) Experimental Results: Induced a high level of γ-H2AX. Caused a significant increase in the ER stress-related protein(p-PERK, p-eIF2α, ATF 4, and CHOP) expression. The level of Bcl-2 was downregulated. |
| Animal Protocol |
Animal/Disease Models: Male BALB/c nude mice (20 to 25 g) injected with A549/CDDP[1]
Doses: 12.40 mg/kg Route of Administration: IV; every 7 days for 28 days Experimental Results: The tumor growth inhibition (TGI) values Dramatically increased to 65.9%. |
| References |
| Molecular Formula |
C23H28CL3N3O6PT
|
|---|---|
| Appearance |
Typically exists as solid at room temperature
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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 |
| 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
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|---|---|
| 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
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