| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Necrosis inducer 1 (compound Au-1) (48 hours) exhibited potent cytotoxicity against a variety of cancer cell lines, with the highest activity against CT-26 cells (IC50 = 1.03 μM) [1]. Necrosis inducer 1 (0.5–2 μM; 24–48 hours) inhibited TrxR activity in CT-26 cells in vitro in a concentration- and time-dependent manner [1]. Necrosis inducer 1 (0.5–2 μM; 24 hours) induced concentration-dependent accumulation of reactive oxygen species (ROS) in CT-26 cells [1]. Necrosis inducer 1 (0.5–4 μM; 24–48 hours) triggered ROS-mediated necroptosis, the main cell death pathway in CT-26 cells, characterized by upregulation of necroptosis-related proteins, increased Annexin V−/PI+ cells, PI uptake, and LDH release [1]. Necrosis inducer 1 (1-2 μM; 24 hours) can induce necrotizing apoptosis-dependent immunogenic cell death (ICD) in CT-26 cells, characterized by concentration-dependent exposure to extracellular calreticulin (ecto-CRT), ATP release and HMGB1 release [1].
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| ln Vivo |
Necrosis inducer 1 (compound Au-1) (10 mg/kg; intravenous injection; twice; 48-hour interval between administrations) showed an intratumoral growth inhibition rate (IRT) of 74.2% against in situ CT-26 tumors and an IRT of 83.9% against distal CT-26 tumors, while maintaining mouse body weight [1]. Necrosis inducer 1 (10 mg/kg; intravenous injection; every two days for 24 days) showed an IRT of 43.1%, while when used in combination with anti-PD-1 antibody, the IRT reached 66.2%. It remodels the tumor immune microenvironment by activating CD8+ and CD4+ helper T cells and reducing regulatory T cells, while maintaining mouse body weight [1].
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| Animal Protocol |
Animal/Disease Models:BALB/c (4 weeks old, sex unknown, subcutaneously inoculated with CT-26 cells to establish primary and distant metastatic tumors) [1]
Doses: 10 mg/kg Route of Administration: Intravenous injection; twice at 48-hour intervals Experimental Results: The tumor growth inhibition rate (IRT) of primary tumors reached 74.2%. The IRT of distant metastatic tumors reached 83.9%. Body weight remained stable during treatment. Animal/Disease Models:BALB/c (4 weeks old, sex unknown, subcutaneously inoculated with CT-26 cells to establish a tumor, tumor volume approximately 50 mm³) [1] Doses: 10 mg/kg Route of Administration: Intravenous injection; every 48 hours Experimental Results: Monotherapy achieved an intratumoral response rate (IRT) of 43.1%. Combined therapy with anti-PD-1 antibody achieved an IRT of 66.2%. Body weight remained stable during treatment. The proportion of tumor-infiltrating CD3+CD8+ T cells increased from 0.83% to 3.57%. The proportion of CD3+CD8+CD38+ T cells increased from 10.03% to 37.68%, and the proportion of CD3+CD8+Ki67+ T cells increased from 30.44% to 48.20%. The proportions of CD8+ T cells expressing TNF-α, IFN-γ, and granzyme B increased to 17.66%, 38.00%, and 23.64%, respectively. The proportion of tumor-infiltrating CD3+CD4+ T cells increased from 0.79% to 5.25%. The proportion of helper T cells (CD4+CD185+) increased from 7.63% to 18.18%. The proportion of immunosuppressive regulatory T cells (CD3+CD4+Foxp3+) decreased from 18.83% to 8.60%. Increased CD3+CD8+ T cell infiltration was observed in the spleen, lymph nodes, and peripheral blood. |
| References |
| Molecular Formula |
C25H28AUF6N2O2PS2
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|---|---|
| Molecular Weight |
794.56
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
F[P-](F)(F)(F)(F)F.CCCCN(C1=[S][Au+]2(C3=CC=CC=C3C4=[N]2C=CC5=C4C=C6C(OCO6)=C5)S1)CCCC
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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 | 1.2586 mL | 6.2928 mL | 12.5856 mL | |
| 5 mM | 0.2517 mL | 1.2586 mL | 2.5171 mL | |
| 10 mM | 0.1259 mL | 0.6293 mL | 1.2586 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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