| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| Other Sizes |
| Targets |
SKI-349 targets two distinct cellular components: sphingosine kinase 1/2 (SPHK1/2) and microtubules (via inhibition of microtubule assembly, MDA). SPHK1/2 are enzymes that produce sphingosine-1-phosphate (S1P), a lipid signaling molecule involved in cell proliferation, survival, and migration. Microtubules are key components of the cytoskeleton essential for cell division. By inhibiting both, SKI-349 disrupts critical pathways for cancer cell growth.
|
|---|---|
| ln Vitro |
In vitro, SKI-349 exhibits anticancer activity by inhibiting the vitality and invasion of liver cells. It also inhibits the AKT/mTOR signaling pathway. These activities contribute to its antiproliferative effects. Specific IC50 values are not detailed in the available literature.
|
| ln Vivo |
In vivo activity data for SKI-349 are not available in the current scientific literature. Its anticancer activity has been characterized in vitro, and no animal model studies have been described.
|
| Enzyme Assay |
In vitro enzyme or receptor binding assay protocols for SKI-349 would typically involve measuring its inhibition of sphingosine kinase 1 and 2 using radiolabeled or mass spectrometry-based assays. Its effects on microtubule assembly can be assessed using tubulin polymerization assays.
|
| Cell Assay |
In vitro cell-based assay protocols for SKI-349 involve treating cancer cell lines, such as liver cancer cells, with the compound. Cell viability, invasion, and signaling pathway modulation (e.g., AKT/mTOR) are assessed using standard assays like MTT, Transwell invasion assays, and Western blot.
|
| Animal Protocol |
In vivo animal experimental protocols for SKI-349 have not been reported. Based on its in vitro anticancer activity, potential xenograft models could be used to evaluate its efficacy.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of SKI-349 have not been characterized in published studies. Its molecular formula is C25H26N6O5S, and its molecular weight is 522.58.
|
| Toxicity/Toxicokinetics |
Toxicological data for SKI-349 are not available in the current literature. It is intended for research use only and not for human use.
|
| References |
|
| Additional Infomation |
SKI-349 is a research-grade compound used as a dual-targeted inhibitor of SPHK1/2 and microtubule assembly for cancer research. It has not entered clinical trials and is not approved for any therapeutic indication. Its mechanism of action involves inhibiting sphingosine kinase and disrupting microtubule dynamics, leading to inhibition of the AKT/mTOR pathway and cancer cell growth. The compound is available exclusively for research purposes.
|
| Molecular Formula |
C19H19N3O4S
|
|---|---|
| Molecular Weight |
385.436863183975
|
| Exact Mass |
385.109
|
| CAS # |
727686-80-8
|
| PubChem CID |
1512282
|
| Appearance |
Light yellow to yellow solid powder
|
| LogP |
4.6
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
27
|
| Complexity |
490
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
COC1=CC=C(C=C1)NC2=NC(=C(S2)C(=O)C3=CC(=C(C=C3)OC)OC)N
|
| InChi Key |
OWBQCPZBRPKYKE-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C19H19N3O4S/c1-24-13-7-5-12(6-8-13)21-19-22-18(20)17(27-19)16(23)11-4-9-14(25-2)15(10-11)26-3/h4-10H,20H2,1-3H3,(H,21,22)
|
| Chemical Name |
[4-amino-2-(4-methoxyanilino)-1,3-thiazol-5-yl]-(3,4-dimethoxyphenyl)methanone
|
| 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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
DMSO :~125 mg/mL (~324.30 mM; with sonication)
|
|---|---|
| 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 | 2.5944 mL | 12.9722 mL | 25.9444 mL | |
| 5 mM | 0.5189 mL | 2.5944 mL | 5.1889 mL | |
| 10 mM | 0.2594 mL | 1.2972 mL | 2.5944 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.