| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
GN-604 (72 hours) inhibited the proliferation of HUH-7, HepG2, HT-29, MDA-MB-231, A549 and CDDP-resistant A549/CDDP cancer cells with IC50 values ranging from 5.32 μM to 9.03 μM. It was highly selective for tumors, had low toxicity to HUVEC cells (IC50 = 29.56 μM), and had the potential to overcome CDDP resistance [1]. GN-604 (10 μM; 24 hours) inhibited the migration of MDA-MB-231 cells better than CDDP or GNS561 alone, with a migration rate of 37.4% [1]. GN-604 (10-20 μM; 2 weeks) inhibited the colony formation of MDA-MB-231 cells in a dose-dependent manner, with 20 μM showing better inhibitory effects than 10 μM [1]. GN-604 (10-20 μM; 24 h) induced apoptosis in MDA-MB-231 cells in a dose-dependent manner, with an apoptosis rate of 15.8% at 10 μM and 33.6% at 20 μM [1]. GN-604 (10 μM; 24 h) induced S-phase arrest in MDA-MB-231 cells [1]. GN-604 (10 μM; 24 h) downregulated the expression of PPT1 and upregulated the level of LC3B-II in MDA-MB-231 cells, thereby disrupting lysosomal function and inhibiting autophagy flux [1]. GN-604 (10 μM; 24 h) upregulated the expression of γ-H2AX in MDA-MB-231 cells, indicating that it induced DNA double-strand breaks [1]. GN-604 (10 μM; 12 h) can induce lysosomal dysfunction in MDA-MB-231 cells, manifested as increased LysoTracker Red fluorescence intensity and increased lysosomal volume [1]. GN-604 (10 μM; 12 h) can disrupt lysosomal acidification in MDA-MB-231 cells, manifested as a change in acridine orange fluorescence ratio [1]. GN-604 (0.25 μM; 12 h) can increase intracellular platinum accumulation in MDA-MB-231 cells by 1.8 times compared to the same concentration of cisplatin (CDDP) [1]. GN-604 (10-20 μM; 12 h) induces DNA strand breaks in MDA-MB-231 cells in a dose-dependent manner, with the damage at 20 μM concentration being greater than that at 10 μM concentration [1].
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|---|---|
| ln Vivo |
GN-604 (14–28 mg/kg; intravenous injection; once a week; 24 days) showed dose-dependent antitumor efficacy in MDA-MB-231 xenograft mice [1].
|
| Cell Assay |
Cell migration assay [1]
Cell Types: MDA-MB-231 Tested Concentrations: 10 μM Incubation Duration: 24 hours Experimental Results: The migration rate of MDA-MB-231 cells was limited to 37.4%, which was more effective than CDDP alone (43.6%) or GNS561 alone (41.2%), but slightly lower than the combination of GNS561 and CDDP (28.3%). |
| Animal Protocol |
Animal/Disease Models:BALB/c nude mice (female, 5 weeks old, 16-18 g)[1]
Doses: 14.0 mg/kg; 28.0 mg/kg Route of Administration: Intravenous injection; once a week; for 24 days Experimental Results: The tumor growth inhibition rate (TGI) in the 14.0 mg/kg dose group was 63.65%. The TGI in the 28.0 mg/kg dose group increased to 72.88%, which was higher than the TGI in the GNS561 + cisplatin combination group. No significant weight loss was observed within 24 days. Histopathological analysis of major organs (heart, liver, spleen, lung, kidney) showed no significant abnormalities. At a dose of 28.0 mg/kg, significant morphological changes in tumor tissue were induced, including cell deformation, necrosis and karyorrhization. The expression of γ-H2AX (a DNA damage marker) was significantly upregulated and the expression of PPT1 was significantly downregulated in tumor tissues, and this effect was enhanced with increasing dose. |
| References |
| Molecular Formula |
C31H37CLN8O6PT
|
|---|---|
| Molecular Weight |
848.21
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
ClC(C=C1)=CC=C1CNC2=NC3=CC=CC=C3C(N4CCC(NC(CCC(N/N=C5CC(C([O-][Pt+2]([NH3])([NH3])[O-]6)=O)(C6=O)C/5)=O)=O)CC4)=C2
|
| HS Tariff Code |
2934.99.9001
|
| 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
|
|---|---|
| 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 | 1.1790 mL | 5.8948 mL | 11.7895 mL | |
| 5 mM | 0.2358 mL | 1.1790 mL | 2.3579 mL | |
| 10 mM | 0.1179 mL | 0.5895 mL | 1.1790 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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