SKI-178
Modify Date: 2024-01-14 09:11:58
SKI-178 structure
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Common Name | SKI-178 | ||
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| CAS Number | 1259484-97-3 | Molecular Weight | 394.42400 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C21H22N4O4 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of SKI-178SKI-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 drug sensitive and multi-drug resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines[1][2]. |
| Name | N'-[1-(3,4-dimethoxyphenyl)ethylidene]-3-(4-methoxyphenyl)-1H-pyrazole-5-carbohydrazide |
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| Description | 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 drug sensitive and multi-drug resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines[1][2]. |
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| Related Catalog | |
| In Vitro | SKI-178 (5 μM; 24 hours)-induced apoptotic cell death correlates with prolonged Bcl-2 phosphorylation[1]. Apoptosis Analysis[1] Cell Line: HL-60 cells Concentration: 5 μM Incubation Time: 24 hours 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. |
| In Vivo | SKI-178 (20mg/kg; retro-orbital injection under isoflurane anesthesia) inhibits leukemic progression in the MLL-AF9 model[3]. Animal Model: MLL-AF9 mouse model (leukemic mice)[3] Dosage: 20 mg/kg Administration: Retro-orbital injection under isoflurane anesthesia; three times per week for 1 and 3 weeks 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). |
| References |
| Molecular Formula | C21H22N4O4 |
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| Molecular Weight | 394.42400 |
| Exact Mass | 394.16400 |
| PSA | 97.83000 |
| LogP | 3.64740 |