| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Dyrk1A-IN-15 (compound FC-2) (0-100 nM) is a reversible ATP competitive inhibitor whose inhibitory effect can be overcome by higher concentrations of ATP [1]. Dyrk1A-IN-15 (5-20 µM, 72 h treatment) primarily targets DYRK1A in the GBM cell line U87MG [1]. Dyrk1A-IN-15 (5-10 µM, 24 h treatment) inhibits the invasive ability of the GBM cell line U87MG by targeting DYRK1A [1]. Dyrk1A-IN-15 (1-10 µM, 20 h treatment) accelerates EGFR destabilization, thereby leading to lysosomal degradation of EGFR-dependent glioblastoma cell line U87MG [1].
|
|---|---|
| ln Vivo |
Dyrk1A-IN-15 (2 mg/kg, intraperitoneal injection, once daily for 30 days) inhibited tumor growth and prolonged the animal cycle in a subcutaneous xenograft model induced by U87MG or U87MG-DYRK1A KO cells (1×106 cells) [1].
|
| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: U87MG Tested Concentrations: 5, 10, 20 µM Incubation Duration: 72 h Experimental Results: Was resistant to the mutant but the mutant retained its kinase activity, when DYRK1A-knockout clones were rescued with the DYRK1A wild-type and the F238L-M240R double mutant[1]. Reduced neurosphere size and number only in the populations rescued with wild-type DYRK1A, but not in those expressing the F238L-M240R mutant[1]. Not decreased neurosphere proliferation, unlike the DYRK1A knockout clones in DYRK2 and DYRK3-knockout clones[1]. Cell Invasion Assay[1] Cell Types: U87MG Tested Concentrations: 5 or 10 µM Incubation Duration: 24 h Experimental Results: Reduced invasion of U87MG cells in a dose-dependent manner[1]. Did not observe any significant reduction of invasion in cells rescued with the DYRK1A F238L-M240R mutant as opposed to rescue with DYRK1A wild type[1]. Western Blot Analysis[1] Cell Types: U87MG Tested Concentrations: 1 or 10 µM Incubation Duration: 20 h Experimental Results: Observed a reduction in total EGFR and ERK phosphorylation levels in U87MG DYRK1A-knockout and U87MG cell lines. Induced the accumulation of EGFR when lysosomal degradation was inhibited by BaFA1. Increased EGFR degradation, a phenotype also observed in DYRK1A-knockout cells. |
| Animal Protocol |
Animal/Disease Models: U87MG or U87MG-DYRK1A KO cells (1 x 106) induced- NuJ nude mice[1]
Doses: 2 mg/kg Route of Administration: i.p., daily for 30 days Experimental Results: Observed the tumors substantially smaller. Failed to develop any tumors in the the DYRK1A-knockout line cohort. Had markedly lower EGFR levels. |
| References |
| Molecular Formula |
C14H9NO4S
|
|---|---|
| Molecular Weight |
287.29
|
| CAS # |
1448757-02-5
|
| 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 | 3.4808 mL | 17.4040 mL | 34.8080 mL | |
| 5 mM | 0.6962 mL | 3.4808 mL | 6.9616 mL | |
| 10 mM | 0.3481 mL | 1.7404 mL | 3.4808 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
