Multi-kinase-IN-2
Multi-kinase-IN-2 (compound 7h) is an orally active and potent angiokinase inhibitor. Multi-kinase-IN-2 exhibits excellent inhibitory activity against angiokinases including VEGFR-1/2/3, PDGFRα/β, and FGFR-1, as well as LYN and c-KIT kinases. Multi-kinase-IN-2 significantly attenuates phosphorylation of AKT and ERK proteins. Multi-kinase-IN-2 induces cell apoptosis. Multi-kinase-IN-2 shows anticancer activity.
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- CAS No.: 2095628-21-8
- Formule: C34H35N5O3
- Masse moléculaire:561.67
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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
- Pureté et documentation
- Références
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Activité biologique
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VEGFR-3 6.3 ± 0.5 nM (IC50) |
VEGFR-2 6.5 ± 0.9 nM (IC50) |
VEGFR-1 31 ± 2.1 nM (IC50) |
PDGFRα 7.0 ± 0.1 nM (IC50) |
PDGFRβ 9.9 ± 0.7 nM (IC50) |
FGFR1 23 ± 2.5 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| Sf9 | IC50 |
7 nM
Compound: 7h
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Inhibition of N-terminal GST-tagged human recombinant PDGFRalpha D842I mutant expressed in baculovirus-infected Sf9 cells using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition measured after 1 hr by mobilit
Inhibition of N-terminal GST-tagged human recombinant PDGFRalpha D842I mutant expressed in baculovirus-infected Sf9 cells using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition measured after 1 hr by mobilit
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[PMID: 32305182] |
Multi-kinase-IN-2 (compound 7h) (0-10 μM, 14 days) potently inhibits colony formation of HT-29, MKN74, and HepG2 cancer cells[1].
Multi-kinase-IN-2 (0-3 μM, 24 h) significantly attenuates phosphorylation of AKT and ERK proteins[1].
Multi-kinase-IN-2 (0-3 μM, 72 h) induces apoptosis of HT-29, MKN74, and HepG2 cell[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, HepG2, and MKN74 cells
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Concentration:0, 0.2, 0.5, 1, and 2 μM or 0, 0.3, 1, 3, and 10 μM
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Incubation Time:14 days
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Result:Exhibited excellent activity in inhibition of colony formations in a dose-dependent manner, with remarkable activity at 1 µM concentration.
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Cell Line:HT-29 and HepG2
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Concentration:0, 0.2, 0.5, 1, and 2 μM or 0, 0.3, 1, 3, and 10 μM
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Incubation Time:24 h
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Result:Suppressed the phosphorylation of AKT (Ser473) in a dose-dependent manner with a significant inhibition of ERK (Thr202/Tyr204) phosphorylation at 3 μM.
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Cell Line:HT-29, MKN74, and HepG2 cells
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Concentration:0, 0.3, 1, and 3 μM
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Incubation Time:72 h
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Result:Triggered severe apoptosis of HT-29, MKN74, and HepG2 cells in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female nu/nu mice (4-6 weeks old, HT-29 human colon cancer xenograft model)[1]
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Dosage:100 mg/kg
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Administration:Orally, once daily for 18 days
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Result:Displayed mild inhibition of tumor growth, with tumor growth inhibition (TGI) value of 13.39%.
Chemical Information
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CAS No. 2095628-21-8
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Masse moléculaire 561.67
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Formule C34H35N5O3
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SMILES
O=C(C1=CC(NC/2=O)=C(C=C1)C2=C(NC3=CC=C(N4C(C)=CC=C4CN5CCN(C)CC5)C=C3)/C6=CC=CC=C6)OC
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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-2 Related Classifications
HY-150026 Related Classifications
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