FLT3-IN-34
FLT3-IN-34 is a FLT3 inhibitor, with an IC50 value of 1.4 nM. FLT3-IN-34 blocks the phosphorylation of FLT3 and its downstream signaling molecules AKT and ERK1/2. FLT3-IN-34 induces concentration-dependent G0/G1 phase arrest and mild apoptosis in FLT3-ITD-positive MV4-11 cells. FLT3-IN-34 shows potent anti-proliferative activity against FLT3-ITD-positive MV4-11 cells (IC50 = 14.95 nM) and MOLM-13 (IC50 = 18.5 nM). FLT3-IN-34 can be used for the study of FLT3-positive acute myeloid leukemia (AML).
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- CAS. Nr.: 3020729-11-4
- Formel: C23H23N5O3
- Molecular Weight:417.46
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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
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
FLT3-IN-34 (Compound ZY12) exhibits excellent inhibitory potency against FLT3-ITD kinase, with an IC50 value of 1.4 nM[1].
FLT3-IN-34 shows potent antiproliferative activity against FLT3-ITD-positive MV4-11 cells (IC50 = 14.95 nM) and MOLM-13 (IC50 = 18.5 nM)[1].
FLT3-IN-34 (5-20 nM, 24 h) concentration-dependently induces G0/G1 phase arrest of MV4-11 cells and induces MV4-11 cell apoptosis[1].
FLT3-IN-34 (5-20 nM) significantly blocks the phosphorylation of FLT3, AKT, and ERK1/2 in MV4-11 and MOLM-13 cells, inhibiting the FLT3 signaling pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4-11 cells
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Concentration:5, 10, 20 nM
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Incubation Time:24 h
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Result:Induced G0/G1 phase arrest of MV4–11 cells and decreases the percentage of cells in S and G2/M phases.
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Cell Line:MV4-11 cells
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Concentration:5, 10, 20 nM
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Incubation Time:24 h
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Result:Induced MV4–11 cell apoptosis.
| Species | Dose | Route | T1/2 | Cmax | AUC0-∞ | MRT |
|---|---|---|---|---|---|---|
| Rat[1] | 30 mg/kg | p.o. | 16.341 h | 3.665 ng/mL | 50.420 ng·h/mL | 15.984 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MV4-11 cells was subcutaneously implanted into the mid-lateral axilla of 4-6 weeks old BALB/c-nu mice[1]
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Dosage:30 mg/kg
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Administration:p.o., once daily, 10 days
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Result:Failed to obviously inhibit tumor growth (TGI=8.55%) in mice bearing MV4-11 subcutaneous xenografts.
Chemical Information
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CAS. Nr. 3020729-11-4
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Molecular Weight 417.46
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Formel C23H23N5O3
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SMILES
O=C(NC1=CC=C(C(C2=CN=C3C=C(C)C=CN32)=O)C=C1)NC4=NOC(C(C)(C)C)=C4
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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)
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