| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
ICD inducer-2 (compound 17) (1.25–5 μM; 60 min) inhibited purified tubulin polymerization in a dose-dependent manner [1]. ICD inducer-2 (0.2–25 μM; 2 h) bound to colchicine binding sites on tubulin in A549 cells [1]. ICD inducer-2 (10–20 nM; 48 h) disrupted the microtubule network in A549 cells at concentrations of 10 and 20 nM [1]. ICD inducer-2 (20–80 nM; 12 h) effectively induced intracellular cell death (ICD) in A549 cells [1]. ICD inducer-2 (8–64 nM; 12–24 h) exhibited immunostimulatory activity in vitro and reduced the viability of A549 cells co-cultured with Jurkat cells [1]. ICD inducer-2 (48 h) showed broad-spectrum anti-proliferative activity against a variety of cancer cell lines, with IC50 values ranging from 8 ± 3 nM (MCF-7) to 47 ± 12 nM (A549/TxR), and could overcome paclitaxel resistance in A549/TxR cells, with an RI value of 4.7 [1]. ICD inducer-2 (5-20 nM; 48 h) could induce dose-dependent G2/M phase arrest in A549 cells, with corresponding arrest rates of 20.16%, 32.83% and 40.30%, respectively, and could regulate cell cycle regulatory proteins [1]. ICD inducer-2 (5-20 nM; 48 h) could induce mitochondrial-mediated apoptosis in A549 cells in a dose-dependent manner, increase late apoptosis and regulate the expression of apoptosis-related proteins [1]. ICD inducer-2 (5-20 nM; 24 h) could inhibit the migration of A549 cells in a dose-dependent manner [1]. ICD inducer-2 (5-20 nM; 8 h) can dose-dependently inhibit tubular formation in HUVEC cells [1].
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|---|---|
| ln Vivo |
ICD inducer-2 (compound 17) (5-15 mg/kg; intravenous injection; every two days; for 28 days) achieved dose-dependent tumor growth inhibition in a paclitaxel-resistant A549/TxR xenograft mouse model, with an inhibition rate of up to 82.0%, and no significant organ toxicity was observed at the maximum tested dose [1]. ICD inducer-2 (10-15 mg/kg; intravenous injection; every two days; for 14 days) achieved dose-dependent tumor growth inhibition in a Lewis lung cancer xenograft mouse model, with an inhibition rate of up to 81.6%, and effectively activated the anti-tumor immune response by increasing T cell infiltration and the production of pro-inflammatory cytokines, and had good safety at the tested dose [1].
|
| Cell Assay |
Western Blot Analysis [1]
Cell Types: A549 cells Tested Concentrations: 0.2, 1, 5, 25 μM Incubation Duration: 2 hours Experimental Results: Effectively inhibited the formation of EBI/β-tubulin complex bands, confirming the binding to the colchicine binding site on tubulin. Immunofluorescence [1] Cell Types: A549 cells Tested Concentrations: 10, 20 nM Incubation Duration: 48 hours Experimental Results: It induced significant microtubule network depolymerization, characterized by structural disorder and weakened fluorescence signal. At a concentration of 20 nM, the induced disruption was more severe than that caused by colchicine. Cell viability assay [1] Cell Types: A549 cells, Jurkat cells Tested Concentrations: 8, 16, 32, 64 nM Incubation Duration: 12-24 hours Experimental Results: Compared with the A549 monoculture group, the viability of A549 cells in the co-culture group was significantly reduced in a dose-dependent manner, indicating that it has the potential for immunostimulation.
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| Animal Protocol |
Animal/Disease Models:Male BALB/c-nu nude mice carrying A549/TxR xenograft tumors [1]
Doses: 5 mg/kg; 10 mg/kg; 15 mg/kg Route of Administration: Intravenous injection; every two days; for 28 days Experimental Results: Tumor growth inhibition rates in the 5, 10, and 15 mg/kg dose groups were 67.3%, 77.1%, and 82.0%, respectively. The tumor growth inhibition rate in the 10 mg/kg dose group was 77.1%, significantly higher than that of the same dose of paclitaxel (17.6%). No significant toxicity to major organs was observed at the maximum dose of 15 mg/kg. Animal/Disease Models:C57BL/6N mice, Lewis lung cancer xenograft model [1] Doses: 10 mg/kg; 15 mg/kg Route of Administration: Intravenous injection; every two days; for 14 days Experimental Results: The tumor growth inhibition rate was 72.4% in the 10 mg/kg dose group and 81.6% in the 15 mg/kg dose group. The tumor growth inhibition rate of 72.4% in the 10 mg/kg dose group was superior to that of the same dose of paclitaxel (64.2%). At the 10 mg/kg dose, the proportions of CD4+ and CD8+ T cells in the tumor tissue increased to 7.008% and 7.439%, respectively, which were significantly higher than those in the blank control group (3.334% and 3.658%) and slightly higher than those in the paclitaxel group (6.627% and 6.559%). At a dose of 15 mg/kg, the proportions of CD4+ and CD8+ T cells in tumor tissue increased to 9.239% and 8.604%, respectively. Serum levels of IFN-γ, IL-2, and IL-12 were significantly elevated, and higher than in the paclitaxel group at a dose of 10 mg/kg. At a dose of 10 mg/kg, it induced significant exposure of calreticulin and release of HMGB1 in tumor cells, with a stronger effect than in the paclitaxel group. At a dose of 15 mg/kg, no significant changes in body weight or significant toxicity to major organs and tissues were observed. |
| References |
| Molecular Formula |
C22H15N3O2S
|
|---|---|
| Molecular Weight |
385.44
|
| CAS # |
3069681-35-9
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| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
N#CC1=C(NC2=CC(C3=CC=CS3)=CC=C2)C4=CC5=C(C=C4N=C1)OCCO5
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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)
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| 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5944 mL | 12.9722 mL | 25.9444 mL | |
| 5 mM | 0.5189 mL | 2.5944 mL | 5.1889 mL | |
| 10 mM | 0.2594 mL | 1.2972 mL | 2.5944 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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