| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
ALK degrader 2 (Compound J26) (72 h) showed antiproliferative activity in H3122 cells (IC50 = 25 nM)[1]. ALK degrader 2 (0.015-5 μM, 24 h) degraded EML4-ALK levels in H3122 cells (DC50 = 8 nM) and nucleophosphorus protein (NPM)-ALK protein levels in SU-DHL-1 cells (DC50 = 102 nM)[1]. ALK degrader 2 (0.01-0.5 μM, 24 h) induced significant S-phase cell cycle arrest and apoptosis in H3122 cells[1]. ALK degrader 2 (0.5 μM, 24 h) mediates ALK degradation via the Hsp70 chaperone and ubiquitin-proteasome pathway, without involving E3 ligases (CRBN, TTC3, ARK2N)[1].
|
|---|---|
| ln Vivo |
ALK degrader 2 (Compound J26) (10 mg/kg, researcher, single dose) significantly reduced EML4-ALK protein levels in tumor tissue in female BALB/c nude mice with H3122 xenografts for 24 hours and continued to be absorbed for up to 72 hours [1]. ALK degrader 2 (20 mg/kg, so-called simple or 5-10 mg/kg, research report, once a day for 21 days) showed antitumor activity in mice with H3122 xenografts [1].
|
| Cell Assay |
Apoptosis Analysis[1]
Cell Types: H3122 cells Tested Concentrations: 0.01, 0.05, 0.5 μM Incubation Duration: 24 h Experimental Results: Induced apoptosis in H3122 cells. Cell Cycle Analysis[1] Cell Types: H3122 cells Tested Concentrations: 0.01, 0.05, 0.5 μM Incubation Duration: 24 h Experimental Results: Induced significant S-phase cell cycle arrest in H3122 cells. |
| Animal Protocol |
Animal/Disease Models: H3122 cells (1 × 106 in appropriate volume) were subcutaneously implanted into the right flanks of 4-week-old female BALB/c nude mice to establish H3122 xenograft tumor models[1]
Doses: 20 mg/kg (p.o.) or 5, 10 mg/kg (i.v.) Route of Administration: once every other day for 21 days Experimental Results: Achieved tumor growth inhibition. Showed no significant changes in body weight and no other signs of toxicity. Significantly reduced EML4-ALK and phosphorylated ALK (p-ALK) protein levels in tumor tissues. Induced significant tumor cell apoptosis. |
| References |
| Molecular Formula |
C40H48N6O2
|
|---|---|
| Molecular Weight |
644.85
|
| Appearance |
Typically exists as solids 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 | 1.5507 mL | 7.7537 mL | 15.5075 mL | |
| 5 mM | 0.3101 mL | 1.5507 mL | 3.1015 mL | |
| 10 mM | 0.1551 mL | 0.7754 mL | 1.5507 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
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