| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
ALK/ROS1-IN-5 (0-100 μM, 72 h) showed excellent inhibitory activity against H2228, H1975 and H460 cells [1]. ALK/ROS1-IN-5 (10 μM) showed significant inhibitory activity against members of the tyrosine kinase family, including EGFR, AKT1, FGFR1 and ERK1 [1]. ALK/ROS1-IN-5 (10 μM) showed significant inhibitory activity against ALK and ROS1 kinases, with inhibition rates of 94.34% and 94.27%, respectively [1]. ALK/ROS1-IN-5 (1-2 μM, 24 h) inhibited the migration of H2228 cells in a dose-dependent manner [1]. ALK/ROS1-IN-5 (1-2 μM, 24 h) induced apoptosis and cell cycle arrest in H2228 cells in a dose-dependent manner [1]. ALK/ROS1-IN-5 (1-2 μM, 24 h) can induce apoptosis in H2228 cells in a dose-dependent manner [1]. ALK/ROS1-IN-5 (0.1-0.5 μM, 24 h) can reduce the phosphorylation levels of ALK and ERK in a dose-dependent manner [1].
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|---|---|
| ln Vivo |
ALK/ROS1-IN-5 (60, 120 mg/kg, orally, once daily for 7 days) showed no significant toxicity in mouse biochemical blood samples [1]. ALK/ROS1-IN-5 (10 mg/kg, orally, once daily for 35 days) showed significant antitumor activity [1]. ALK/ROS1-IN-5 (5-25 mg/kg, orally, once daily for 14 days) had minimal effect on reticulopenia (RET) [1]. Tumor volume growth rate of ALK/ROS1-IN-5 (25-50 mg/kg, orally, once daily for 21 days) was lower than that of the positive control group [1]. ALK/ROS1-IN-5 reduced the expression of Ki67, Bcl2, Caspase 3 and PCNA in a dose-dependent manner [1].
|
| Animal Protocol |
Animal/Disease Models:KM mice [1].
Doses: 60, 120 mg/kg. Route of Administration: Oral, once daily for 7 days. Experimental Results: No obvious toxicity was observed. Animal/Disease Models:Tumor-bearing nude mouse H2228[1]. Doses: 10 mg/kg Route of Administration: Oral administration, once daily for 35 days Experimental Results: Compared with carboplatin monotherapy, the combination therapy with 37.5 mg/kg once weekly significantly improved the antitumor effect (TGI was 94.7%, compared to 69.7% for carboplatin monotherapy). No significant weight loss was observed during the study. Animal/Disease Models:Tumor-bearing nude mouse H2228[1]. Doses: 5, 25 mg/kg. Route of Administration: Oral, once daily for 14 days. Experimental Results: Minimal effect on reticulopenia (RET). No significant weight loss was observed during the study. Animal/Disease Models:Tumor-bearing nude mouse H2228[1]. Doses: 25, 50 mg/kg Route of Administration: Oral administration, once every 48 hours for 21 days Experimental Results: Tumor growth rate was lower than that of the positive control group. Tumor inhibition rate was greater than 30%. |
| References |
| Molecular Formula |
C32H28F2N4O3
|
|---|---|
| Molecular Weight |
554.59
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
FC1=CC(F)=CC(CC2=CC=C(NN=C3NC(C4=CC=C(C5=CC=C(OC)C=C5)C=C4N6CCOCC6)=O)C3=C2)=C1
|
| 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 | 1.8031 mL | 9.0157 mL | 18.0313 mL | |
| 5 mM | 0.3606 mL | 1.8031 mL | 3.6063 mL | |
| 10 mM | 0.1803 mL | 0.9016 mL | 1.8031 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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