| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
ZM484 (72 hours) showed potent antiproliferative activity against three cancer cell lines, HCT116, SJSA-1, and A549, with IC50 values of 0.03, 0.97, and 0.11 μM, respectively [1]. ZM484 (1.56–50 μM, 72 hours) showed minimal cytotoxicity against the non-cancerous MRC-5 cell line [1]. ZM484 (3.125–100 μM, 30 minutes) did not show hemolytic activity at a concentration of 100 μM [1]. ZM484 (50 μM, 0–24 hours) maintained a concentration of over 95% for 24 hours and showed excellent stability even in acidic buffer solutions with pH values of 2 or 5 [1]. ZM484 (25–100 nM, 8 days) significantly reduced the colony-forming ability of HCT116 cells [1]. ZM484 (0.195-200 μM, 15 min) inhibited TOP1 activity in a concentration-dependent manner, maintaining its potency even at concentrations as low as 0.195 μM [1]. ZM484 (50-100 nM, 4 h) upregulated p53 and MDM2 protein levels in a concentration-dependent manner [1]. ZM484 (10-40 nM, 24 h) effectively induced cell cycle arrest in HCT116 cells during the S and G2 phases [1]. ZM484 (10-640 nM, 48 h) exhibited potent, concentration-dependent pro-apoptotic activity in cancer cells, accompanied by a dose-dependent decrease in caspase-3 and Bcl-2 expression levels [1].
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|---|---|
| ln Vivo |
ZM484 (10 mg/kg, intraperitoneal injection, every other day for 12 days) showed significant tumor growth inhibition in the HCT116 xenograft model [1].
|
| Cell Assay |
Cell Cytotoxicity Assay[1]
Cell Types: HCT116 cells Tested Concentrations: 25, 50, and 100 nM Incubation Duration: 8 days Experimental Results: Significantly reduced the colony formation ability of HCT116 cells at concentrations of 25, 50, and 100 nM. Western Blot Analysis[1] Cell Types: HCT116 cells Tested Concentrations: 50 and 100 nM Incubation Duration: 4 h Experimental Results: Increased p53 and MDM2 protein levels in a concentration-dependent manner. Exhibited more activity than Idasanutlin at 50 and 100 nM for p53 protein upregulation. Cell Cycle Analysis[1] Cell Types: HCT116 cells Tested Concentrations: 10 and 40 nM Incubation Duration: 24 h Experimental Results: Induced a dose-dependent increase in the S phase (29.8% and 43.3% at 10 and 40 nM, respectively) and G2 phase (20.9% and 28.3%) cell populations. Apoptosis Analysis[1] Cell Types: HCT116 cells Tested Concentrations: 40, 160, and 640 nM Incubation Duration: 48 h Experimental Results: Induced significant apoptosis in a concentration-dependent manner, with apoptotic rates of 11.6%, 16.8%, and 25.8% at concentrations of 40, 160, and 640 nM, respectively. Induced apoptosis more effectively than Idasanutlin or the vehicle control. Decreased the expression levels of caspase-3, Bcl-2 in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models: Female BALB/c nude mice (4-6 weeks) subcutaneously injected with HCT116 cells[1]
Doses: 10 mg/kg Route of Administration: i.p., every other day for 12 days Experimental Results: Exhibited the highest tumor growth inhibition (TGI of 81.07%) among the tested groups, surpassing the positive controls Idasanutlin (25 mg/kg, i.g., qd, TGI = 68.59%) and Irinotecan (50 mg/kg, i.p., qw, TGI = 64.01%). |
| References |
| Molecular Formula |
C67H72CL2F2N6O15S2
|
|---|---|
| Molecular Weight |
1374.35
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| Appearance |
Typically exists as solids at room temperature
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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 | 0.7276 mL | 3.6381 mL | 7.2762 mL | |
| 5 mM | 0.1455 mL | 0.7276 mL | 1.4552 mL | |
| 10 mM | 0.0728 mL | 0.3638 mL | 0.7276 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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