| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
ALK-IN-37 (compound CO4) (48 hours) selectively inhibited the proliferation of ALK-overexpressing H2228 cells (IC50 = 0.10 μM) and ALK-positive Karpas299 cells (IC50 = 0.53 μM), with weak activity against ALK-negative A549 cells and no activity against WML2 cells [1]. ALK-IN-37 (50-200 nM; 14 days) inhibited the colony formation of H2228 cells in a dose-dependent manner, with the colony formation efficiency decreasing to 36.3% at 200 nM [1]. ALK-IN-37 (50-200 nM; 24-48 hours) inhibited the migration of H2228 cells in a dose-dependent manner, with a concentration of 200 nM reducing the scratch healing rate to 28.5% after 48 hours [1]. ALK-IN-37 (100-200 nM; 24 hours) inhibited the invasion of H2228 cells in a dose-dependent manner, and a concentration of 200 nM reduced the relative invasion area to 36.6% [1]. ALK-IN-37 (50-200 nM; 24 hours) induced cell cycle arrest in the G0/G1 phase of H2228 cells in a dose-dependent manner, and a concentration of 200 nM increased the proportion of cells in the G0/G1 phase to 85.0% [1]. ALK-IN-37 (50-200 nM; 24 hours) induced apoptosis in H2228 cells in a dose-dependent manner, and treatment with 200 nM increased the proportion of apoptotic cells to 55.9% [1]. ALK-IN-37 (50-200 nM) inhibited ALK phosphorylation and its downstream STAT3/AKT signaling pathway in H2228 cells in a dose-dependent manner, with the strongest inhibitory effect at 200 nM [1].
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|---|---|
| ln Vivo |
ALK-IN-37 (compound CO4) (10-30 mg/kg; oral; daily; 15 days) showed dose-dependent potent antitumor efficacy and ALK-targeting inhibition in BALB/c nude mice carrying H2228 NSCLC xenografts, with activity superior to crizotinib at 30 mg/kg [1].
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| Animal Protocol |
Animal/Disease Models:BALB/c nude mice (female) [1]
Doses: 10 mg/kg; 20 mg/kg; 30 mg/kg Route of Administration: Oral; Daily; 15 days Experimental Results: Showed dose-dependent tumor growth inhibition, with significantly reduced tumor weight in all treatment groups compared to the vector control group. The relative p-ALK/ALK level decreased to approximately 85% of the vector control group in the 10 mg/kg dose group, approximately 70% in the 20 mg/kg dose group, and approximately 35% in the 30 mg/kg dose group, with a reduction greater than that in the 30 mg/kg crizotinib group. At the 10 mg/kg dose, the p-ALK positive area decreased to approximately 30% of the vector control group; at the 20 mg/kg dose, it decreased to approximately 18%; and at the 30 mg/kg dose, it decreased to approximately 8%, with a reduction greater than that in the 30 mg/kg crizotinib group. Compared with the control group, there was no significant difference in body weight among the groups, and no treatment-related pathological damage was observed in the major organs. |
| References |
| Molecular Formula |
C19H16N6O
|
|---|---|
| Molecular Weight |
344.37
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
O=C(C1=CC(C2=CC=CC(N3C=NN=C3)=C2)=NN1)NC4=CC=CC(C)=C4
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| 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)
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| 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 | 2.9039 mL | 14.5193 mL | 29.0385 mL | |
| 5 mM | 0.5808 mL | 2.9039 mL | 5.8077 mL | |
| 10 mM | 0.2904 mL | 1.4519 mL | 2.9039 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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