SphK1-IN-2
SphK1-IN-2 is a potent, selective SphK1 inhibitor with IC50 values of 19.81 nM and ＞10 μM for SphK1 and SphK2, respectively. SphK1-IN-2 exhibits anti-proliferative activities and induces cell cycle arrest and apoptosis. SphK1-IN-2 can be used for cancer research.
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- CAS. Nr.: 3031483-60-7
- Formel: C27H30BrNO4S
- Molecular Weight:544.50
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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SphK1 19.81 nM (IC50) |
SphK2 ＞10 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| HT-29 | IC50 |
3.85 μM
Compound: 28
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Antiproliferative activity against human HT-29 cells incubated for 72 hrs by SRB assay
Antiproliferative activity against human HT-29 cells incubated for 72 hrs by SRB assay
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[PMID: 35439002] |
| MCF7 | IC50 |
4 μM
Compound: 28
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Antiproliferative activity against human MCF7 cells incubated for 72 hrs by SRB assay
Antiproliferative activity against human MCF7 cells incubated for 72 hrs by SRB assay
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[PMID: 35439002] |
| MDA-MB-231 | IC50 |
7.14 μM
Compound: 28
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Antiproliferative activity against human MDA-MB-231 cells for 72 hrs by SRB assay
Antiproliferative activity against human MDA-MB-231 cells for 72 hrs by SRB assay
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[PMID: 35439002] |
| SW480 | IC50 |
4 μM
Compound: 28
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Antiproliferative activity against human SW480 cells incubated for 72 hrs by SRB assay
Antiproliferative activity against human SW480 cells incubated for 72 hrs by SRB assay
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[PMID: 35439002] |
SphK1-IN-2 (4-24 μM; 72 hours; cancer cell lines) has anti-proliferative activity on cancer cells[1].
SphK1-IN-2 (10-30 μM; 48 hours; HT-29 cells and MDA-MB-231 cells) induces G0/G1 phase arrest and apoptosis in colon cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT-29, SW480, MDA-MB231 and MCF-7 cells
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Concentration:4-24 μM
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Incubation Time:72 hours
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Result:Had inhibitory activity against HT-29 and MDA-MB-231 with IC50 of 3.85 and 7.14 μM, respectively.
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Cell Line:HT-29 cells and MDA-MB-231 cells
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Concentration:10 and 30 μM
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Incubation Time:72 hours
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Result:Arrestd cell cycle at G0/G1 phase and reduced the expression of cyclin A, cyclin E1, cyclin D1, and CDK6.
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Cell Line:HT-29 cells and MDA-MB-231 cells
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Concentration:10 and 30 μM
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Incubation Time:48 hours
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Result:Induced cell apoptosis in a dose-dependent manner.
SphK1-IN-2 (2-50 mg/kg; p.o., i.p. and i.v.; female BALB/c nude mice) exhibits a long half-life (T1/2=8.13 h) and high plasma exposure (AUClast = 8061 h*ng/mL)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c nude mice[1]
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Dosage:2, 20 and 50 mg/kg(Pharmacokinetic Analysis)
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Administration:Oral administration, intraperitoneal injection and intravenous injection
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Result:
1.19 admin. p.o. i.p. i.v. Tmax (min) 0.83 0.18 Cmax (ng/mL) 171 78582 AUClast (h*ng/mL) 242 8061 408 T1/2 (h) 8.13 4.20 2.23 CL_obs (mL/min/kg) 81.10 F (%) 2.38 79.00
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Animal Model:Female BALB/c nude mice[1]
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Dosage:50 and 100 mg/kg
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Administration:Intraperitoneal injection; daily; for 14 days
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Result:Inhibited the growth of HT29 tumors at a dose of 50 mg/kg and inhibited the growth of MDA-MB-231 breast tumors in a dose-dependent manner.
Chemical Information
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CAS. Nr. 3031483-60-7
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Molecular Weight 544.50
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Formel C27H30BrNO4S
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SMILES
OC[C@@H]1N(CC2=CC=C(COC3=CC(CS(=O)(C4=CC=CC=C4)=O)=C(Br)C(C)=C3)C=C2)CCC1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
SphK1-IN-2 Related Classifications
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