| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
JAK2-IN-14 (Compound 15au) (0.01-5 μM, 24 h) significantly induced cell cycle arrest at the G2/M phase and apoptosis in BaF3-JAK2V617F and HEL cells in a dose-dependent manner [1]. JAK2-IN-14 (0.05-1 μM, 2 h) effectively inhibited the phosphorylation of JAK2 and its downstream signaling molecule STAT5 in BaF3-JAK2V617F and HEL cells [1].
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|---|---|
| ln Vivo |
JAK2-IN-14 (Compound 15au) (7.5-40 mg/kg, po, once daily for 13-28 days) significantly inhibited tumor growth in BaF3-JAK2V617F and HEL cell xenograft models [1].
|
| Cell Assay |
Cell Cycle Analysis[1]
Cell Types: BaF3-JAK2V617F and HEL cells Tested Concentrations: 10, 50, 100, 500 and 1000 nM Incubation Duration: 24 h Experimental Results: Blocked the progression of tumor cells at the G2/M phase, leading to a decrease in the proportions of cells in the G1/G0 and G2 phases. Western Blot Analysis[1] Cell Types: BaF3-JAK2V617F and HEL cells Tested Concentrations: 10, 50, 100, 500 and 1000 nM Incubation Duration: 2 h Experimental Results: Reduced p-JAK2 and p-STAT5 levels concentration-dependently. |
| Animal Protocol |
Animal/Disease Models: BaF3-JAK2V617F allogeneic transplantation model established in BALB/c-nude mice[1]
Doses: 7.5, 15 and 30 mg/kg Route of Administration: Oral administration (p.o.), once daily for 13 days Experimental Results: Demonstrated significant therapeutic efficacy, reducing spleen weight by 24.1%, 26.4%, and 40.5% at doses of 7.5, 15, and 30 mg/kg, respectively Animal/Disease Models: HEL cells xenograft model was established in 6-week-old male BALB/c nude mice[1] Doses: 20 and 40 mg/kg Route of Administration: Oral administration (p.o.), once daily for 28 days Experimental Results: Significantly inhibited subcutaneous tumor growth. did not induce observable body weight loss during the experimental period. |
| References |
| Molecular Formula |
C26H33N7O
|
|---|---|
| Molecular Weight |
459.59
|
| CAS # |
3087335-24-5
|
| Appearance |
Typically exists as solids at room temperature
|
| 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 | 2.1759 mL | 10.8793 mL | 21.7585 mL | |
| 5 mM | 0.4352 mL | 2.1759 mL | 4.3517 mL | |
| 10 mM | 0.2176 mL | 1.0879 mL | 2.1759 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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