| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Anti-TNBC drug-15 (compound 14) (100 nM-50 μM; 72 h) effectively inhibited MDA-MB-231, A549, HCT-116, A549/CDDP, MDA-MB-231/CDDP and MCF-10A cells, with IC50 values of 2.38, 3.77, 4.36, 4.29, 2.25 and 12.17, respectively [1]. Anti-TNBC drug-15 (5 μM; 12-24 h) significantly increased platinum accumulation in MDA-MB-231 cells and cisplatin-resistant MDA-MB-231/CDDP cells, strongly induced DNA damage in MDA-MB-231/CDDP cells, and increased the expression levels of γ-H2AX and p53 and the olive tail moment value in the comet assay [1]. Anti-TNBC drug-15 (5 μM; 24 h) induces apoptosis in cisplatin-resistant MDA-MB-231/CDDP cells by upregulating pro-apoptotic proteins and downregulating anti-apoptotic proteins Bcl-2, and disrupts the mitochondrial membrane potential of the cells [1]. Anti-TNBC drug-15 (5 μM; 24 h) inhibits the cystine/glutamate transporter-glutathione peroxidase axis in cisplatin-resistant MDA-MB-231/CDDP cells by downregulating the expression of xCT and GPX4 [1]. Anti-TNBC drug-15 (5 μM; 24–72 h) induces cell death in cisplatin-resistant MDA-MB-231/CDDP cells through ferroptosis [1]. Anti-TNBC drug-15 (5 μM; 12–24 h) disrupts the GSH redox system and induces widespread lipid peroxidation in cisplatin-resistant MDA-MB-231/CDDP cells [1]. Anti-TNBC drug-15 (5 μM; 24 h) inhibited the migration and invasion of cisplatin-resistant MDA-MB-231/CDDP cells [1].
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| ln Vivo |
Anti-TNBC drug-15 (compound 14) (5.0–16.7 mg/kg; intravenous injection; every 7 days; 28 days) dose-dependently inhibited the growth of cisplatin-resistant triple-negative breast cancer tumors in xenograft mice, with a TGI rate of 63.4% at a dose of 16.7 mg/kg and minimal systemic toxicity [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: MDA-MB-231, A549, HCT-116, A549/CDDP, MDA-MB-231/CDDP, MCF-10A cells Tested Concentrations: 100 nM, 500 nM, 1 μM, 5 μM, 10 μM, 50 μM Incubation Duration: 72 hours Experimental Results: The highest cytotoxicity was observed in all tested cell lines, with IC50 values of 2.38 μM (MDA-MB-231), 3.77 μM (A549), 4.36 μM (HCT-116), 4.29 μM (A549/CDDP), 2.25 μM (MDA-MB-231/CDDP), and 12.17 μM, respectively. μM (MCF-10 A). The resistance factor (RF1) was 1.14 (A549/CDDP and A549), the RF2 was 0.95 (MDA-MB-231/CDDP and MDA-MB-231), and the selectivity factor (SF) was 5.11 (MCF-10 A and MDA-MB-231). Apoptosis analysis [1] Cell Types: MDA-MB-231/CDDP cells Tested Concentrations: 5 μM Incubation Duration: 24 hours Experimental Results: 52.87% apoptosis rate was induced in MDA-MB-231/CDDP cells, which was higher than that ligand 8 (22.95%), oxaliplatin (38.4%) and the combination of ligand 8 and oxaliplatin (46.23%). Western Blot Analysis [1] Cell Types: MDA-MB-231/CDDP Cells Concentration: 5 μM Incubation Duration: 24 hours Experimental Results: The expression of pro-apoptotic proteins Cyt c, Bax, cleaved caspase 3 and cleaved caspase 9 was upregulated, with protein densities relative to β-actin reaching ~0.5, ~0.75, ~0.85 and ~0.7, respectively. The expression of anti-apoptotic protein Bcl-2 was downregulated, with a protein density relative to β-actin of approximately 0.05. The expression of cystine/glutamate transporter (xCT) and glutathione peroxidase 4 (GPX4) proteins was significantly downregulated, with protein densities relative to β-actin reaching approximately 0.3 and approximately 0.1, respectively.
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| Animal Protocol |
Animal/Disease Models:BALB/c nude mice (female) [1]
Doses: 5.0 mg/kg; 16.7 mg/kg Route of Administration: Intravenous injection; every 7 days; for 28 days Experimental Results: The tumor growth inhibition rate (TGI) in the 5.0 mg/kg dose group was 44.6%. The tumor growth inhibition rate (TGI) in the 16.7 mg/kg dose group was 63.4%. During the 28-day treatment period, there was no significant difference in body weight between the groups compared with the saline control group, indicating low systemic toxicity. Extensive nuclear loss was induced in tumors (16.7 mg/kg dose group, H&E staining). Decreased proliferative activity was shown in tumors (16.7 mg/kg dose group, Ki-67 staining). |
| References |
| Molecular Formula |
C34H39CLN6O13PTS
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|---|---|
| Molecular Weight |
1002.31
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
O=C(O[Pt](OC1=O)([NH2][C@H]2[C@H]3CCCC2)([NH2]3)(Cl)OC1=O)CCCC(OCCOC4=CC=C(/N=N/C5=CC=C(S(=O)(NC6=NC=CC=C6)=O)C=C5)C=C4C(OC)=O)=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 | 0.9977 mL | 4.9885 mL | 9.9770 mL | |
| 5 mM | 0.1995 mL | 0.9977 mL | 1.9954 mL | |
| 10 mM | 0.0998 mL | 0.4988 mL | 0.9977 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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