| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Cytotoxin-platinum(IV) prodrug-1 (compound CP12) (72 hours) effectively inhibited the activity of H226, SW1990, HepG2 and MDA-MB-231 tumor cells, with IC50 values of 0.09, 0.15, 0.21 and 0.61 μM, respectively, and the selectivity for tumor cells was much higher than that for normal PUMC-HUVEC-T1 cells [1]. Cytotoxin-platinum(IV) prodrug-1 (100 μM; 12-72 hours) showed high stability in PBS, RPMI-1640 medium and rat plasma when incubated at 37°C [1]. Cytotoxin-platinum(IV) prodrug-1 (100 μM; 16 hours) was reductively activated in H226 cells, releasing the cytotoxin derivative CYT-COOH [1]. Cytotoxin-platinum(IV) prodrug-1 (1 μM; 24 h) effectively inhibited the colony formation of H226 cells and effectively killed H226 cells [1]. Cytotoxin-platinum(IV) prodrug-1 (1 μM; 24 h) can effectively inhibit the migration and apoptosis of H226 cells[1]. Cytotoxin-platinum(IV) prodrug-1 (1 μM; 12 h) can induce strong S-phase cell cycle arrest in H226 cells, resulting in 62.19% of cells accumulating in the S phase and reducing the expression of cyclin D1[1]. Cytotoxin-platinum(IV) prodrug-1 (1 μM; 24 h) can induce endoplasmic reticulum stress in H226 cells, activate the IP3R1-GRP75-VDAC1 axis, and cause mitochondrial calcium overload, thereby exerting its antitumor activity[1]. Cytotoxin-platinum(IV) prodrug-1 (1 μM; 24 h) can induce mitochondrial dysfunction in H226 cells, characterized by reduced ATP production, collapse of mitochondrial membrane potential (MMP), increased reactive oxygen species (ROS) production, release of cytochrome C, and mitochondrial morphology disruption[1]. Cytotoxin-platinum(IV) prodrug-1 (1 μM; 24 h) can activate the cGAS-STING pathway in H226 cells, upregulate key proteins in the pathway and promote IL-6 secretion[1]. Cytisine-platinum(IV) prodrug-1 (1 μM; 24 h) can effectively induce immunogenic cell death in H226 cells, characterized by increased CRT exposure, increased release of HMGB1, LDH and ATP and decreased PD-L1 expression[1].
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| ln Vivo |
Cytotoxin-platinum (IV) prodrug-1 (compound CP12) (2-4 mg/kg platinum; intravenous injection; once every 3 days; for a total of 6 doses) can effectively inhibit the growth of H226 lung cancer tumors in nude mice, and has no obvious hepatotoxicity or nephrotoxicity, and has minimal effect on body weight[1]. Cytotoxin-platinum (IV) prodrug-1 (2-4 mg/kg platinum; intravenous injection; once every 3 days; for a total of 6 doses) can effectively inhibit the growth of LLC lung cancer tumors in immune-normal mice, while activating the cGAS-STING pathway, inducing immunogenic cell death, and enhancing cytotoxic T cell infiltration, thereby reshaping the tumor microenvironment[1].
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| Cell Assay |
Cell migration assay [1]
Cell Types: H226 Tested Concentrations: 1 μM Incubation Duration: 24 hours Experimental Results: Significantly inhibited the migration of H226 cells, resulting in a wound healing rate of only 2.44%. Apoptosis analysis [1] Cell Types: H226 Tested Concentrations: 1 μM Incubation Duration: 24 h Experimental Results: A high apoptosis rate of 80.4% was induced in H226 cells. Cell cycle analysis [1] Cell Types: H226 Tested Concentrations: 1 μM Incubation Duration: 12 hours Experimental Results: The H226 cell cycle was significantly arrested in the S phase, with 62.19% of the cells in the S phase, and the transition from the S phase to the G2 phase was completely blocked. The expression of cyclin D1 was reduced.
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| Animal Protocol |
Animal/Disease Models:BALB/c nude mice (male, 4-6 weeks old, 18 g, xenograft model derived from H226 cells) [1]
Doses: 2, 4 mg/kg platinum Route of Administration: Intravenous injection; once every 3 days; 6 times in total Experimental Results: Tumor growth inhibition rate (TGI) reached 59.3%. Tumor growth inhibition rate (TGI) reached 72.7%. No significant weight loss was observed; the weight of the low-dose group was comparable to that of the control group, while the weight of the high-dose group showed an increasing trend. No significant abnormalities were caused in the liver, lungs, or kidneys. Compared with cisplatin (CDDP), the accumulation of platinum in tumor tissue was significantly higher, while the accumulation of platinum in kidney tissue was significantly lower. The area of necrosis in tumor tissue was induced to increase in a concentration-dependent manner. Animal/Disease Models:C57BL/6 (male, 5 weeks old, 18 g, LLC cell-derived xenograft model) [1] Doses: 2, 4 mg/kg Pt Route of Administration: Intravenous injection; once every 3 days; 6 doses in total Experimental Results: Tumor growth inhibition rate (TGI) reached 69.1%. Tumor growth inhibition rate (TGI) reached 81.1%. No significant weight loss was observed. The cGAS-STING pathway in tumor tissue was potently activated in a dose-dependent manner. The exposure of calreticulin (CRT) and the release of high-mobility group box 1 (HMGB1) in tumor tissue were significantly increased. The infiltration of CD3+ and CD8+ T cells in the tumor was significantly increased compared with the control group and the cisplatin group. |
| References |
| Molecular Formula |
C29H51CL2N5O6PT
|
|---|---|
| Molecular Weight |
831.74
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
[NH3][Pt](Cl)(Cl)([NH3])(OC(CCCC(N1C[C@](C2=CC=CC(N2C[C@@]3(C1)[H])=O)(C3)[H])=O)=O)OC(NCCCCCCCCCCCC)=O
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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 | 1.2023 mL | 6.0115 mL | 12.0230 mL | |
| 5 mM | 0.2405 mL | 1.2023 mL | 2.4046 mL | |
| 10 mM | 0.1202 mL | 0.6011 mL | 1.2023 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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