SKI-I
Based on 1 Customer Validation
SKI-I is a potent and selective inhibitor of human sphingosine kinase (SK), with an IC50 of 1.2 μM for ST-hSK. SKI-I also inhibits hERK2 (IC50=11 μM). SKI-I induces apoptosis in tumor cell lines.
For research use only. We do not sell to patients.
- Purity: 99.73%
- CAS No.: 306301-68-8
- Formula: C25H18N4O2
- Molecular Weight:406.44
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Biological Activity
IC50: 1.2 μM (ST-hSK); 11 μM (hERK2)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
3.8 μM
Compound: 4, SKI-I
|
Cytotoxicity against human A549 cells after 72 hrs by SRB assay
Cytotoxicity against human A549 cells after 72 hrs by SRB assay
|
[PMID: 20598402] |
| HeLa | IC50 |
1 μM
Compound: 4, SKI-I
|
Cytotoxicity against human HeLa cells after 72 hrs by SRB assay
Cytotoxicity against human HeLa cells after 72 hrs by SRB assay
|
[PMID: 20598402] |
| MCF-10A | IC50 |
4.1 μM
Compound: 4, SKI-I
|
Cytotoxicity against human MCF10A cells after 72 hrs by SRB assay
Cytotoxicity against human MCF10A cells after 72 hrs by SRB assay
|
[PMID: 20598402] |
| MDA-MB-231 | IC50 |
4.4 μM
Compound: 4, SKI-I
|
Cytotoxicity against human MDA-MB-231 cells after 72 hrs by SRB assay
Cytotoxicity against human MDA-MB-231 cells after 72 hrs by SRB assay
|
[PMID: 20598402] |
| MEF | IC50 |
5 μM
Compound: 4, SKI-I
|
Cytotoxicity against MEF after 72 hrs by SRB assay
Cytotoxicity against MEF after 72 hrs by SRB assay
|
[PMID: 20598402] |
| MIA PaCa-2 | IC50 |
4.8 μM
Compound: 4, SKI-I
|
Cytotoxicity against human MIAPaCa2 cells after 72 hrs by SRB assay
Cytotoxicity against human MIAPaCa2 cells after 72 hrs by SRB assay
|
[PMID: 20598402] |
| NCI-H226 | IC50 |
5.7 μM
Compound: 4, SKI-I
|
Cytotoxicity against human NCI-H226 cells after 72 hrs by SRB assay
Cytotoxicity against human NCI-H226 cells after 72 hrs by SRB assay
|
[PMID: 20598402] |
| NCI-H441 | IC50 |
2 μM
Compound: 4, SKI-I
|
Cytotoxicity against human H441 cells after 72 hrs by SRB assay
Cytotoxicity against human H441 cells after 72 hrs by SRB assay
|
[PMID: 20598402] |
| NCI-H460 | IC50 |
3.2 μM
Compound: 4, SKI-I
|
Cytotoxicity against human H460 cells after 72 hrs by SRB assay
Cytotoxicity against human H460 cells after 72 hrs by SRB assay
|
[PMID: 20598402] |
| U-87MG ATCC | IC50 |
1 μM
Compound: 4, SKI-I
|
Cytotoxicity against human U87MG cells after 72 hrs by SRB assay
Cytotoxicity against human U87MG cells after 72 hrs by SRB assay
|
[PMID: 20598402] |
Chemical Information
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CAS No. 306301-68-8
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Appearance Solid
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Molecular Weight 406.44
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Formula C25H18N4O2
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Color Off-white to light yellow
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SMILES
O=C(C1=NNC(C2=CC=C3C=CC=CC3=C2)=C1)N/N=C/C4=C5C=CC=CC5=CC=C4O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 100 mg/mL (246.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. French KJ, et, al. Discovery and evaluation of inhibitors of human sphingosine kinase. Cancer Res. 2003 Sep 15;63(18):5962-9. [Content Brief]
[2]. Sharma AK, et, al. Synthesis and bioactivity of sphingosine kinase inhibitors and their novel aspirinyl conjugated analogs. Eur J Med Chem. 2010 Sep;45(9):4149-56. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4604 mL | 12.3019 mL | 24.6039 mL | 61.5097 mL |
| 5 mM | 0.4921 mL | 2.4604 mL | 4.9208 mL | 12.3019 mL | |
| 10 mM | 0.2460 mL | 1.2302 mL | 2.4604 mL | 6.1510 mL | |
| 15 mM | 0.1640 mL | 0.8201 mL | 1.6403 mL | 4.1006 mL | |
| 20 mM | 0.1230 mL | 0.6151 mL | 1.2302 mL | 3.0755 mL | |
| 25 mM | 0.0984 mL | 0.4921 mL | 0.9842 mL | 2.4604 mL | |
| 30 mM | 0.0820 mL | 0.4101 mL | 0.8201 mL | 2.0503 mL | |
| 40 mM | 0.0615 mL | 0.3075 mL | 0.6151 mL | 1.5377 mL | |
| 50 mM | 0.0492 mL | 0.2460 mL | 0.4921 mL | 1.2302 mL | |
| 60 mM | 0.0410 mL | 0.2050 mL | 0.4101 mL | 1.0252 mL | |
| 80 mM | 0.0308 mL | 0.1538 mL | 0.3075 mL | 0.7689 mL | |
| 100 mM | 0.0246 mL | 0.1230 mL | 0.2460 mL | 0.6151 mL |