SKI-178
Based on 1 publication(s) in Google Scholar
SKI-178 is a potent sphingosine kinase-1 (SphK1) and SphK2 inhibitor. SKI-178 is cytotoxic at IC50 concentrations ranging from 1.8 to 0.1 μM in both agent sensitive and multi-agent resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR cells). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines.
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- Purity: 99.29%
- CAS No.: 1259484-97-3
- 화학식: C21H22N4O4
- 분자량:394.42
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) SKI-178
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Biological Activity
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SphK1 |
SphK2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.3 μM
Compound: 20
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Cytotoxicity against human A549 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human A549 cells after 48 hrs by sulforhodamine B assay
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[PMID: 21050755] |
| BXPC-3 | IC50 |
0.2 μM
Compound: 20
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Cytotoxicity against human BxPC3 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human BxPC3 cells after 48 hrs by sulforhodamine B assay
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[PMID: 21050755] |
| HL-60 | IC50 |
0.2 μM
Compound: 20
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Cytotoxicity against human HL60 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human HL60 cells after 48 hrs by sulforhodamine B assay
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[PMID: 21050755] |
| HL-60 | IC50 |
0.2 μM
Compound: 20
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Cytotoxicity against VCR-resistance human HL60 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against VCR-resistance human HL60 cells after 48 hrs by sulforhodamine B assay
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[PMID: 21050755] |
| HL-60 | IC50 |
470 nM
Compound: SKI-178
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Cytotoxicity against human HL-60 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human HL-60 cells assessed as reduction in cell viability after 48 hrs by MTT assay
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[PMID: 32736077] |
| KG-1a | IC50 |
0.5 μM
Compound: 20
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Cytotoxicity against human KG1a cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human KG1a cells after 48 hrs by sulforhodamine B assay
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[PMID: 21050755] |
| MCF7 | IC50 |
1.3 μM
Compound: 20
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Cytotoxicity against human MCF7 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human MCF7 cells after 48 hrs by sulforhodamine B assay
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[PMID: 21050755] |
| MCF7 | IC50 |
1.8 μM
Compound: 20
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Cytotoxicity against human tamoxifen-resistant MCF7 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human tamoxifen-resistant MCF7 cells after 48 hrs by sulforhodamine B assay
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[PMID: 21050755] |
| MIA PaCa-2 | IC50 |
0.1 μM
Compound: 20
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Cytotoxicity against human MIAPaCa2 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human MIAPaCa2 cells after 48 hrs by sulforhodamine B assay
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[PMID: 21050755] |
| NCI-H226 | IC50 |
0.3 μM
Compound: 20
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Cytotoxicity against human NCI-H226 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human NCI-H226 cells after 48 hrs by sulforhodamine B assay
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[PMID: 21050755] |
| NCI-H460 | IC50 |
0.3 μM
Compound: 20
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Cytotoxicity against human H460 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human H460 cells after 48 hrs by sulforhodamine B assay
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[PMID: 21050755] |
| PANC-1 | IC50 |
0.1 μM
Compound: 20
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Cytotoxicity against human PANC1 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human PANC1 cells after 48 hrs by sulforhodamine B assay
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[PMID: 21050755] |
| SH-SY5Y | IC50 |
0.3 μM
Compound: 20
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Cytotoxicity against human SH-SY5Y cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human SH-SY5Y cells after 48 hrs by sulforhodamine B assay
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[PMID: 21050755] |
| U-251 | IC50 |
0.5 μM
Compound: 20
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Cytotoxicity against human U251 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human U251 cells after 48 hrs by sulforhodamine B assay
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[PMID: 21050755] |
| U-87MG ATCC | IC50 |
0.6 μM
Compound: 20
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Cytotoxicity against human U87MG cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human U87MG cells after 48 hrs by sulforhodamine B assay
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[PMID: 21050755] |
SKI-178 (5 μM; 24 hours)-induced apoptotic cell death correlates with prolonged Bcl-2 phosphorylation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HL-60 cells
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Concentration:5 μM
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Incubation Time:24 hours
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Result:JNK activity (indicated by phosphorylation at Thr183/Tyr185) increased in a time-dependent manner starting as early as 2 hours continued to increase for at least 24 hours. There was a concomitant increase in apoptotic cell death indicated by the cleavage of caspase-7. Bcl-2 phosphorylation at Ser70 increased with time in response to SKI-178 treatment, reaching maximal levels at 8 hours, which was consistent with the timing of caspase-7 activation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MLL-AF9 mouse model (leukemic mice)[3]
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Dosage:20 mg/kg
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Administration:Retro-orbital injection under isoflurane anesthesia; three times per week for 1 and 3 weeks
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Result:White blood cell (WBC) counts decreased from their initial 104 cells/μL levels and continued to decline after 3 weeks of treatment until they reached normal levels (~4×103 cells/μL).
Chemical Information
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CAS No. 1259484-97-3
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Appearance Solid
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분자량 394.42
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화학식 C21H22N4O4
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Color White to off-white
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SMILES
O=C(C1=CC(C2=CC=C(OC)C=C2)=NN1)N/N=C(C3=CC=C(OC)C(OC)=C3)\C
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
용액&용해도
DMSO : 50 mg/mL (126.77 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. 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. 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (6.34 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
순도&문서
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Data Sheet (274 KB)
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SDS (614 KB)
- English - EN (614 KB)
- Français - FR (614 KB)
- Deutsch - DE (614 KB)
- Norwegian - NO (614 KB)
- Español - ES (614 KB)
- Swedish - SV (614 KB)
- Italian - IT (614 KB)
- Korean - KR (614 KB)
- Portuguese - PT (614 KB)
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Handling Instructions (2659 KB)
References
[1]. Hengst JA, et al. SKI-178: A Multitargeted Inhibitor of Sphingosine Kinase and Microtubule Dynamics Demonstrating Therapeutic Efficacy in Acute Myeloid Leukemia Models. Cancer Transl Med. 2017;3(4):109-121. [Content Brief]
[2]. Hengst JA, et al. Development of a sphingosine kinase 1 specific small-molecule inhibitor. Bioorg Med Chem Lett. 2010;20(24):7498-7502. [Content Brief]
[3]. Dick TE, et al. The apoptotic mechanism of action of the sphingosine kinase 1 selective inhibitor SKI-178 in human acute myeloid leukemia cell lines. J Pharmacol Exp Ther. 2015;352(3):494-508. [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. 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 | 2.5354 mL | 12.6768 mL | 25.3537 mL | 63.3842 mL |
| 5 mM | 0.5071 mL | 2.5354 mL | 5.0707 mL | 12.6768 mL | |
| 10 mM | 0.2535 mL | 1.2677 mL | 2.5354 mL | 6.3384 mL | |
| 15 mM | 0.1690 mL | 0.8451 mL | 1.6902 mL | 4.2256 mL | |
| 20 mM | 0.1268 mL | 0.6338 mL | 1.2677 mL | 3.1692 mL | |
| 25 mM | 0.1014 mL | 0.5071 mL | 1.0141 mL | 2.5354 mL | |
| 30 mM | 0.0845 mL | 0.4226 mL | 0.8451 mL | 2.1128 mL | |
| 40 mM | 0.0634 mL | 0.3169 mL | 0.6338 mL | 1.5846 mL | |
| 50 mM | 0.0507 mL | 0.2535 mL | 0.5071 mL | 1.2677 mL | |
| 60 mM | 0.0423 mL | 0.2113 mL | 0.4226 mL | 1.0564 mL | |
| 80 mM | 0.0317 mL | 0.1585 mL | 0.3169 mL | 0.7923 mL | |
| 100 mM | 0.0254 mL | 0.1268 mL | 0.2535 mL | 0.6338 mL |
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