Physicochemical Properties
| CAS # | 2923433-95-6 |
| Appearance | Typically exists as solid at room temperature |
| 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) |
Biological Activity
| ln Vitro | APE1-IN-2 (compound AP1) has the ability to significantly suppress the proliferation of cancerous cells, even those resistant to cisplatin, by up to 18.11 times when compared to cisplatin (HY-17394)[1]. A549 and MCF7 cells have their cell cycle arrested by APE1-IN-2 (500 nM, 24 h)[1]. In A549 cells, APE1-IN-2 (10 μM, 24 h) causes p53-dependent apoptosis[1]. With an IC50 of 45.14 ± 17.37 μM, APE1-IN-2 (0- 250 μM, 72 h) inhibits AP-cutting activity[1]. APE1-IN-2 has the ability to directly inhibit APE1's AP endonuclease activity, which stops miRNA processing and causes the tumor suppressor PTEN to be overexpressed[1]. |
| ln Vivo | On the A549 xenograft model, APE1-IN-2 (compound AP1) (2 mg/kg, IP, once every 3 days for 15 days) shows anticancer effects[1]. |
| Cell Assay |
Cell Proliferation Assay[1] Cell Types: A549 (non-small cell lung cancer), MCF7 (breast cancer), U251 (glioblastoma), A375 (melanoma), PC3 (prostate cancer), and HEP-G2 (hepatocarcinoma) cell lines Tested Concentrations: Incubation Duration: 72 h Experimental Results: Demonstrated more potent antiproliferation effects than Cisplatin (HY- 17394), with IC50 of 0.45 ± 0.03, 0.43 ± 0.03, 4.70 ± 0.14, 0.39 ± 0.03, 5.65 ± 0.21, and 3.53 ± 0.31 μM in A549, MCF7, U251, A375, PC3, and HEP-G2 cell lines respectively. Cell Cycle Analysis[1] Cell Types: A549 and MCF7 cells Tested Concentrations: 500 nM Incubation Duration: 24 h Experimental Results: Induced the most severe S-phase arrest in A549 and MCF7 cells. Cell Proliferation Assay[1] Cell Types: A549 cells Tested Concentrations: 10 μM Incubation Duration: 24 h Experimental Results: Caused apoptosis in approximately 38.7% (22.9% early apoptosis and 15.8% late apoptosis) of cancer cells. Western Blot Analysis[1] Cell Types: A549 and HEK-293T cell lines Tested Concentrations: 0, 16, 40, 100, 250 μM Incubation Duration: 72 h Experimental Results: Signi |
| Animal Protocol |
Animal/Disease Models: BALB/c nude mice (5 week-old, female, 16 ± 2 g of body weight bearing A549 xenograft tumors)[1] Doses: 2 mg/kg Route of Administration: IP, once every 3 days for 15 days Experimental Results: demonstrated a 3.86-fold xenograft tumor inhibitory activity compared to Cisplatin. Did not Dramatically alter the body weight of mice, improving its sufficient safety. |
| References |
[1]. Pt(IV) Prodrug as a Potential Antitumor Agent with APE1 Inhibitory Activity. J Med Chem. 2022 Nov 24;65(22):15344-15357. |
Solubility Data
| 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 (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *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). 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)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL 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). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently. (Please use freshly prepared in vivo formulations for optimal results.) |