| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
ATM-IN-2 (compound 25a) (0-10000 nM, 6-7 days) showed good inhibitory activity against HEL116 and SW620 cells, with IC50 values of 58.2 nM and 66.6 nM, respectively, and effectively inhibited cell colony formation [1]. ATM-IN-2 (1-4 μM, 2 days) enhanced the therapeutic effect of irinotecan by aggravating G2/M phase arrest and promoting apoptosis, and achieved a synergistic antiproliferative effect in HCT116 cells [1]. ATM-IN-2 (0.25-2 μM, 4 hours) significantly inhibited the activation of the ATM signaling pathway in HCT116 and SW620 cells [1].
|
|---|---|
| ln Vivo |
ATM-IN-2 (compound 25a) (15-30 mg/kg, orally, for 14-20 days) produced a synergistic antitumor effect when combined with irinotecan in a mouse xenograft model of cancer treatment [1].
|
| Cell Assay |
Cell cycle analysis [1]
Cell Types: HCT116 cells Tested Concentrations: 1, 2, 4 μM, in combination with irinotecan () Incubation Duration: 2 days Experimental Results: No significant effect on cell cycle when used alone. Concentration-dependently increased the proportion of cells in the G2/M phase while decreasing the proportion of cells in the G0/G1 phase. Apoptosis analysis [1] Cell Types: HCT116 cells Tested Concentrations: 1, 2, 4 μM co-treated with irinotecan Incubation Duration: 2 days Experimental Experimental Results: The apoptosis rate was significantly increased compared with monotherapy. Western Blot Analysis [1] Cell Types: HCT116 and SW620 cells Tested Concentrations: 0.5, 1, and 2 μM in HCT116 cells, and 0.25, 0.5, and 1 μM in SW620 cells Incubation Duration: 4 hours Experimental Results: Reduced phosphorylation levels of ATM-S1981 and p53. Reduced accumulation of γH2AX. |
| Animal Protocol |
Animal/Disease Models: Xenograft models induced by HCT116 or SW620 cells were established in 6-week-old NOD-SCID mice [1].
Doses: In the HCT116 model, 30 mg/kg alone, and 15 mg/kg and 30 mg/kg combined with 2 mg/kg irinotecan were used; in the SW620 model, 45 mg/kg combined with 2 mg/kg irinotecan was used. Route of Administration: Oral (po), HCT116 model lasted 14 days, SW620 model lasted 20 days. Experimental Results: In the HCT116 model, high dose combined with irinotecan showed better antitumor effects. The HCT116 model had good safety, with only slight weight loss observed. The SW620 model showed enhanced dose-dependent inhibition. |
| References |
| Molecular Formula |
C25H21N3O3S
|
|---|---|
| Molecular Weight |
443.52
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
CC(S(=O)(C1=CC=C(C=C1)C2=CN=C3NC=C(C3=C2)C4=CC(C5=CC=CC=C5)=NO4)=O)C
|
| 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 | 2.2547 mL | 11.2734 mL | 22.5469 mL | |
| 5 mM | 0.4509 mL | 2.2547 mL | 4.5094 mL | |
| 10 mM | 0.2255 mL | 1.1273 mL | 2.2547 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
