| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
DNA-PK-IN-16 (compound D11) (48 hours) effectively inhibited the proliferation of LoVo, B16-F10, Jurkat, HL-60, MDA-MB-436 and MDA-MB-231 cancer cells, with IC50 values ranging from 1.6 to 6.9 μM [1]. DNA-PK-IN-16 (1-10 μM; 24 hours) upregulated the expression of γH2A.X in bleomycin (5)-treated LoVo cells in a concentration-dependent manner, indicating impaired DNA damage repair function [1]. DNA-PK-IN-16 (1-10 μM; 24 hours) induced LoVo cell apoptosis in a dose-dependent manner, reduced mitochondrial membrane potential, disrupted cell cycle progression, and inhibited cell migration [1].
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|---|---|
| ln Vivo |
DNA-PK-IN-16 (25-50 mg/kg; orally; once daily; for 15 days) inhibited the growth of LoVo colorectal cancer xenografts in a dose-dependent manner [1]. DNA-PK-IN-16 (50 mg/kg; orally; once daily) inhibited the growth of B16-F10 melanoma (tumor growth inhibition rate 49.2%) and, in synergy with anti-PD-L1 monoclonal antibodies, enhanced antitumor efficacy by increasing CD8+ T cell infiltration (tumor growth inhibition rate 69.6%), while maintaining good safety [1].
|
| Animal Protocol |
Animal/Disease Models:BALB/c nude mice (male, 6-8 weeks old, subcutaneously inoculated with LoVo cells)[1]
Doses: 25 mg/kg; 50 mg/kg Route of Administration: Gavage; once daily; 15 days Experimental Results: The tumor growth inhibition rate (TGI) in the 25 mg/kg dose group was 30.1%. The TGI in the 50 mg/kg dose group was 72.9%. Ki-67 and PCNA (cell proliferation markers) were downregulated in a dose-dependent manner. TUNEL-positive apoptotic cells were upregulated in a dose-dependent manner. γH2A.X signaling (DNA double-strand break marker) in tumor tissue was enhanced in a dose-dependent manner. No significant decrease in body weight or food intake was observed in mice during treatment. |
| References |
| Molecular Formula |
C25H28N8O
|
|---|---|
| Molecular Weight |
456.54
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
C1(C2=CN=C(N=C2)N3CCNCC3)=CC=C(C4=C1)N=CC5=C4N(C6CCOCC6)C7=NCCN57
|
| 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)
|
| 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 | 2.1904 mL | 10.9519 mL | 21.9039 mL | |
| 5 mM | 0.4381 mL | 2.1904 mL | 4.3808 mL | |
| 10 mM | 0.2190 mL | 1.0952 mL | 2.1904 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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