| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
HSND80 (0.1-104 nM, 72 hours) inhibited the growth of MDA-MB-23, MDA-MB-468, 4T1, T47D, MCF-7, HOP-92, NCI-H226, NCI-H522, EKVX, NCI-H322M, A549, NCI-H23, NCI-H460, HOP-62, and KLN205 cells, with IC50 values of 8.8 nM, 18.3 nM, 0.93 nM, 84.2 nM, 18.5 nM, 27 nM, 29.5 nM, 31.6 nM, 38 nM, 57.5 nM, 79.4 nM, 107.2 nM, and 107.2 nM, respectively. The values were 144.5 nM and 360 nM, respectively [1]. HSND80 (200 nM, 30 h) induces G1 phase arrest [1]. HSND80 (0.5-3 μM, 4 h) downregulates the phosphorylation levels of eIF4E (target of MNK1/2) and S6 and eIF4B (target of p70S6K) [1].
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| ln Vivo |
HSND80 (10 mg/kg; orally) can improve oral bioavailability. The maximum concentration of HSND80 in the plasma of male CD1 mice reached 176 ng/mL at 2 hours and decreased to 2.5 ng/mL at 24 hours [1]. HSND80 (15 mg/kg, 30 mg/kg; orally; 5 days of treatment, 2 days off, and 15 days of treatment) can reduce tumor volume in DBA/2 mice [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: MDA-MB-23, MDA-MB-468, 4T1, T47D, MCF-7, HOP-92, NCI-H226, NCI-H522, EKVX, NCI-H322M, A549, NCI-H23, NCI-H460, HOP-62, KLN205 Tested Concentrations: 0.1-104 nM Incubation Duration: 72 hours Experimental Results: Cell viability decreased. Cell cycle analysis [1] Cell Types: MDA-MB-231 Tested Concentrations: 200 nM Incubation Duration: 30 hours Experimental Experimental Results: Induced G1 phase arrest. Western Blot Analysis [1] Cell Types: MDA-MB-231 Tested Concentrations: 0.5 μM, 1 μM, 3 μM Incubation Duration: 4 hours Experimental Results: Phosphorylation levels of eIF4E (target of MNK1/2) and S6 and eIF4B (target of p70S6K) were downregulated. |
| Animal Protocol |
Animal/Disease Models:0.7 x 10⁶ KLN 205 cells/100 μL were subcutaneously injected into 6-8 week old DBA/2 mice, and the mice were given the drug 6 months later [1].
Doses: 15 or 30 mg/kg. Route of Administration: Gavage; 5 days of continuous administration followed by 2 days of withdrawal; for a total of 15 days. Experimental Results: Tumor volume was reduced. Animal/Disease Models:Male CD1 mice [1] Doses: 10 mg/kg Route of Administration: Oral gavage (po), with blood samples taken within 0.25–24 hours. Experimental Results: Oral bioavailability was improved, with peak plasma concentration of 176 ng/mL at 2 hours and decreasing to 2.5 ng/mL at 24 hours. |
| References |
| Molecular Formula |
C33H35F3N8O2
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|---|---|
| Molecular Weight |
632.68
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
O=C(NC1=CC=C(CN2CCN(C)CC2)C(C(F)(F)F)=C1)C3=CN=CC(C#CC4=CN=C5C=CC(N6C[C@H](C)O[C@H](C)C6)=NN54)=C3
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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 | 1.5806 mL | 7.9029 mL | 15.8058 mL | |
| 5 mM | 0.3161 mL | 1.5806 mL | 3.1612 mL | |
| 10 mM | 0.1581 mL | 0.7903 mL | 1.5806 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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