Multi-kinase-IN-15
Multi-kinase-IN-15 is an orally active multi-kinase inhibitor. Multi-kinase-IN-15 inhibits the kinase activity of MNK1, MNK2, ABL1, ABL1 T315I, FLT3, VEGFR2, RET, cKIT, FGFR2, PDGFRα, and PDGFRβ. Multi-kinase-IN-15 dose-dependently reduces phosphorylation of eIF4E and phosphorylated Crkl in tumor cells, and decreases phosphorylation of eIF4E in tumor tissues. Multi-kinase-IN-15 inhibits tumor growth. Multi-kinase-IN-15 can be used for research on chronic myeloid leukemia.
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- CAS No.: 1613168-52-7
- Formule: C31H35F3N6O2
- Masse moléculaire:580.66
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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- Pureté et documentation
- Références
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Activité biologique
Description
IC50 & Target
[1]|
MNK1 2.52 μM (IC50) |
MNK2 16 nM (IC50) |
Abl1 89 nM (IC50) |
ABL-T315I 50 nM (IC50) |
VEGFR2 24 nM (IC50) |
FLT3 20 nM (IC50) |
FGFR2 0.93 μM (IC50) |
Ret 7 nM (IC50) |
PDGFRα 0.672 μM (IC50) |
cKIT 0.888 μM (IC50) |
PDGFRβ 1.803 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HeLa | IC50 |
0.18 μM
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Inhibition of eIF4E Ser209 phosphorylation in human HeLa cells incubated 2 hrs by Alphascreen SureFire assay.
Inhibition of eIF4E Ser209 phosphorylation in human HeLa cells incubated 2 hrs by Alphascreen SureFire assay.
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27011159 |
| K562 | GI50 |
0.058 μM
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Antiproliferative activity against human K562 cells assessed as viability reduction incubated 48 hrs by CellTiter-Glo assay.
Antiproliferative activity against human K562 cells assessed as viability reduction incubated 48 hrs by CellTiter-Glo assay.
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27011159 |
| BV-173 | GI50 |
0.030 μM
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Antiproliferative activity against human BV-173 cells assessed as viability reduction incubated 48 hrs by CellTiter-Glo assay.
Antiproliferative activity against human BV-173 cells assessed as viability reduction incubated 48 hrs by CellTiter-Glo assay.
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27011159 |
| EM-2 | GI50 |
0.015 μM
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Antiproliferative activity against human EM-2 cells assessed as viability reduction incubated 48 hrs by CellTiter-Glo assay.
Antiproliferative activity against human EM-2 cells assessed as viability reduction incubated 48 hrs by CellTiter-Glo assay.
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27011159 |
| KCL-22 | GI50 |
0.050 μM
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Antiproliferative activity against human KCL-22 cells assessed as viability reduction incubated 48 hrs by CellTiter-Glo assay.
Antiproliferative activity against human KCL-22 cells assessed as viability reduction incubated 48 hrs by CellTiter-Glo assay.
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27011159 |
In Vitro
Multi-kinase-IN-15 (0.003-50 μM; 48 h) inhibits proliferation of CML cell lines with GI50 values of 15-58 nM, and a GI50 of 51 nM in eIF4E-overexpressing K562 cells[1].
Multi-kinase-IN-15 (100-1000 nM; 24 h) induces a dose-dependent decrease in phospho-eIF4E and phospho-Crkl in K562 cells overexpressing eIF4E[1].
Multi-kinase-IN-15 (1 μM) inhibits RET (IC50 0.007 μM), FLT3 (0.020 μM), and VEGFR2 (0.024 μM) in cell-free kinase assays, with weaker activity against KIT, PDGFRα, PDGFRβ, and FGFR2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:K562 cells overexpressing eIF4E
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Concentration:100, 500, and 1000 nM
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Incubation Time:24 h
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Result:Reduced phospho-eIF4E dose-dependently.
Reduced phospho-Crkl dose-dependently.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C.B-Igh-1b/IcrTac-Prkd-scid (female, 7-10 weeks old)[1]
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Dosage:100 mg/kg, and 200 mg/kg
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Administration:p.o. (oral gavage); once daily (QD); 14 days
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Result:Inhibited tumor growth in a dose-dependent manner when administered orally once daily for 14 days.
Showed dose-dependent tumor growth inhibition at 100 and 200 mg/kg.
Chemical Information
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CAS No. 1613168-52-7
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Masse moléculaire 580.66
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Formule C31H35F3N6O2
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SMILES
O=C(NC1=CC=C(C(=C1)C(F)(F)F)CN2CCN(CC)CC2)CNC3=CC=C(C=C3)C=4C=NC(=CC4)NC(=O)C5CC5
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Multi-kinase-IN-15 Related Classifications
HY-131571 Related Classifications
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