Kit-IN-3
Kit-IN-3 is a KIT inhibitor with an IC50 of 2.4 nM. Kit-IN-3 targets the wild-type receptor tyrosine kinase, blocks SCF-mediated autophosphorylation, and reduces cellular activity in serum. Kit-IN-3 inhibits the off-target class III receptor tyrosine kinase PDGFRα with an IC50 of 97 nM, is selective for PDGFRα and PDGFRβ, and has no activity against CSF1R and FLT3.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Fòrmula: C21H17F2N5O2
- Peso molecular:409.39
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
Actividad biológica
Descripciòn
IC50 & Target
[1]|
KIT 2.4 nM (IC50) |
PDGFRα 97 nM (IC50) |
PDGFRβ |
In Vitro
Kit-IN-3 (Compound 69) (50 min) inhibits SCF-mediated KIT autophosphorylation in M07e cells with pKIT IC50 = 7.5 nM under serum-free conditions and 200 nM in 100% serum[1].
Kit-IN-3 (1 h) is a potent biochemical KIT inhibitor (IC50 = 2.4 nM) with high selectivity over PDGFRβ, CSF1R, and FLT3 in HTRF assays[1].
Kit-IN-3 (0.5 μM; different time points) has low intrinsic clearance in rat and human hepatocytes (rat CLint = 3.76; human CLint <2.70 μL/min/106 cells)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
Chemical Information
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Peso molecular 409.39
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Fòrmula C21H17F2N5O2
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SMILES
O=C(NC1=CC=C(OC)C=C1)CC2=C(F)C=C(C3=CC4=NC(N)=NN4C=C3)C=C2F
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)