FD2024
FD2024 is a pan-PIM kinase inhibitor with IC50 values of 0.17 nM, 1.86 nM, and 0.38 nM against PIM-1, PIM-2, and PIM-3, respectively. FD2024 induces cell apoptosis. FD2024 inhibits the phosphorylation of mTOR, p70S6K, S6, 4EBP1, and BAD proteins. FD2024 exhibits anti-acute myeloid leukemia activity. FD2024 can be used in studies related to acute myeloid leukemia.
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- Formule: C22H22F2N6O2
- Masse moléculaire:440.45
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Activité biologique
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Chemical Information
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Activité biologique
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PIM1 0.17 nM (IC50) |
PIM2 1.86 nM (IC50) |
PIM3 0.38 nM (IC50) |
FD2024 potently inhibits PIM-1, PIM-2, and PIM-3 kinases with IC50 values of 0.17 nM, 1.86 nM, and 0.38 nM, respectively[1].
FD2024 (48 h) potently inhibits the proliferation of multiple human AML cell lines, with IC50 values ranging from 0.02 μM (MOLM-13) to 0.25 μM (MOLM-16)[1].
FD2024 (1-5 μM; 48 h) dose-dependently induces apoptosis in human AML cell lines, with significantly higher apoptotic rates at 5 μM compared to 1 μM in both MV-4-11 and EOL-1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV-4-11
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Concentration:1 μM, 5 μM
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Incubation Time:48 h
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Result:Induced apoptosis in 14.9% of MV-4-11 cells at 1 μM.
Induced apoptosis in 83.8% of MV-4-11 cells at 5 μM.
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Cell Line:EOL-1, MV-4-11
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Concentration:0.1, 0.2, 0.5, 1.0, 2.0, 5.0 μM
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Incubation Time:3 h
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Result:Dose-dependently inhibited the phosphorylation of mTOR, p70S6K, S6, 4EBP1, and BAD proteins.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSFG (NOD-PrkdcscidB6-IL2rgnullNh) (male, 6-8 weeks old, intravenous transplantation of luciferase-expressing MV-4-11 cells)[1]
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Dosage:7.5 mg/kg; 15 mg/kg
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Administration:i.p.; daily; 14 days
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Result:Suppressed leukemic progression via reduced in vivo bioluminescence intensity.
Prolonged overall survival to 44 days (all vehicle control mice died by day 36).
Showed no treatment-related organ toxicity in liver, heart, spleen, lungs, and kidneys.
Maintained stable body weight throughout the study period.
Chemical Information
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Masse moléculaire 440.45
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Formule C22H22F2N6O2
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SMILES
FC(C=CC=C1F)=C1C2=NC(C(NC3=C(O[C@@H]4CC[C@@H](N)CC4)C=CN=C3)=O)=C(N)N=C2
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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)
FD2024 Related Classifications
HY-181925 Related Classifications
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