| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
IC50:1.15 nM (ATM)[1]
|
|---|---|
| ln Vitro |
ATM Inhibitor-8 exerts inhibitory effects on breast cancer cells (MCF-7) and colorectal cancer cells (HCT116, SW620) [1]. MCF-7 cell viability can be inhibited by combining ATM Inhibitor-8 (200 nM) with 4.22 μM Etposide and 0.036 μM Irinotecan [1]. ATM Inhibitor-8 (200 nM) in conjunction with 0.22 μM Irinotecan can lower SW620 cell viability and prevent SW620 cell colony formation (0.02 μM) [1].
|
| ln Vivo |
The combination of ATM Inhibitor-8 with Irinotecan (40 mg/kg) (HY-16562) inhibits the growth of tumors in the SW620 mouse model [1]. Balb/c mice exhibit favorable PK values for ATM Inhibitor-8 (10 mg/kg, iv), indicating reduced plasma clearance, increased plasma exposure, and superior oral bioavailability. [1].
|
| Cell Assay |
Western Blot Analysis
Cell Types: HCT116 cell[1] Tested Concentrations: 200 nM Incubation Duration: 4 h Experimental Results: :Inhibted ATM pathway obviously combined with 25 μM Irinotecan. Cell Cycle Analysis Cell Types: HCT116 cell[1] Tested Concentrations: 200 nM Incubation Duration: 48 h Experimental Results: diminished G0/G1 phase cells and increased G0/G1 phase cells with the concentration increase. |
| Animal Protocol |
Animal/Disease Models: Mouse xenograft model of human colon cancer[1].
Doses: 40 mg/kg combined with Irinotecan(40 mg/kg) Route of Administration: ATM Inhibitor-8, 20 or 40 mg/kg, po one time/day for 3 days every week starting 24 h post-irinotecan dosing (40 mg/kg, ip once weekly). Experimental Results: Inhibited tumor growth Dramatically. |
| References |
| Molecular Formula |
C26H34N6O2
|
|---|---|
| Molecular Weight |
462.59
|
| CAS # |
2956666-60-5
|
| 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)
|
| 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 | 2.1617 mL | 10.8087 mL | 21.6174 mL | |
| 5 mM | 0.4323 mL | 2.1617 mL | 4.3235 mL | |
| 10 mM | 0.2162 mL | 1.0809 mL | 2.1617 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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