| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
In cell-free HTRF assays, AK177 inhibited PDGFRA kinase activity with an IC50 value of 9.0 nM[1]. In cell-free HTRF assays, AK177 inhibited KIT kinase activity with an IC50 value of 113.7 nM[1]. In cell-free kinase assays, AK177 inhibited the activity of 49 out of 85 tested kinases[1]. AK177 (0.25–20 μM; 24 h) had a weak induction effect on XBP1 mRNA splicing in MCF-7 cells, with an activation fold change of less than 2 after 24 h of treatment with 20 μM[1]. Even at the highest treatment concentration of 20 μM for 24 h, AK177 (0.25–20 μM; 24 h) did not induce detectable Bloc1s1 mRNA degradation in MCF-7 cells via the RIDD pathway[1]. Even at concentrations as high as 100 μM, AK177 (1–100 μM; 72 hours) did not significantly inhibit the viability of HT-29, MDA-MB-231, and MCF-7 cells after 72 hours of treatment [1].
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|---|---|
| Cell Assay |
Real-time quantitative PCR[1]
Cell Types: MCF-7 human breast cancer cells Tested Concentrations: 0.25, 0.77, 2.22, 6.67 and 20 μM Incubation Duration: 24 hours Experimental Results: At the highest test concentration of 20 μM, the increase in XBP1s mRNA level was less than 2-fold, and the concentration-dependent changes were minimal at all test doses. Bloc1s1 mRNA levels did not change significantly at any test concentration. |
| References |
| Molecular Formula |
C26H28N8O5S
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|---|---|
| Molecular Weight |
564.62
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
CC1=CC(NC2=CC(N3CCN(CC3)C(C4=CC=CC=C4)C(O)=O)=NC(OC5=CC=C(C=C5)S(N)(=O)=O)=N2)=NN1
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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)
|
| 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 | 1.7711 mL | 8.8555 mL | 17.7110 mL | |
| 5 mM | 0.3542 mL | 1.7711 mL | 3.5422 mL | |
| 10 mM | 0.1771 mL | 0.8856 mL | 1.7711 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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