Kit-IN-2
Kit-IN-2 is an orally active and highly selective KIT inhibitor. Kit-IN-2 stabilizes the inactive (DFG-out) conformation of KIT. Kit-IN-2 inhibits mast cell-mediated inflammatory responses by blocking stem cell factor-induced ear swelling and vascular permeability in rats. Kit-IN-2 exhibits favorable pharmacokinetic properties in rats. Kit-IN-2 can be used for studies related to acute allergy.
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- No. CAS: 3080682-14-7
- Fòrmula: C20H17FN6O
- Peso molecular:376.39
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Chemical Information
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Actividad biológica
Descripciòn
In Vitro
Kit-IN-2 (compound 7) potently inhibits the activity of purified KIT kinase in HTRF assays, with an IC50 of 2.8 nM; it suppresses phosphorylated KIT protein in SCF-induced M07e cells, with an IC50 of 14 nM; under physiologically relevant 100% human serum conditions, its IC50 is 0.16 μM[1].
Kit-IN-2 exhibits excellent kinome selectivity, with a selectivity score S (50%) of 0.003 across 371 wild-type kinases, and shows over 350-fold higher selectivity for KIT than ABL2, its only significant off-target kinase[1].
Kit-IN-2 exhibits low potential for drug-drug interactions, with no significant direct or time-dependent inhibitory effects on major human CYP subtypes[1].
Kit-IN-2 (5 μM) exhibits favorable cell permeability and low efflux mediated by P-gp and BCRP[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
| Species | Dose | Route | CL | Vss | MRT | T1/2 | AUC0-∞ | Cmax | F |
|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 0.5 mg/kg | i.v. | 0.28 L/h/kg | 0.91 L/kg | 3.4 h | 2.8 h | / | / | / |
| Rat[1] | 2.0 mg/kg | p.o. | / | / | / | / | 8500 ng·h/mL | 1200 ng/mL | 160 % |
| Mice[1] | 0.5 mg/kg | i.v. | 7.8 L/h/kg | 0.78 L/kg | 0.10 h | 0.11 h | / | / | / |
| Dog[1] | 0.5 mg/kg | i.v. | 0.83 L/h/kg | 0.64 L/kg | 0.81 h | 0.60 h | / | / | / |
| Dog[1] | 2.0 mg/kg | p.o. | / | / | / | / | 2100 ng·h/mL | 760 ng/mL | 76 % |
| Monkey[1] | 0.5 mg/kg | i.v. | 0.37 L/h/kg | 1.7 L/kg | 4.9 h | 6.1 h | / | / | / |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley rat (male, weight 200-250 g)[1]
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Dosage:10 mg/kg
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Administration:p.o.; single dose
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Result:Blocked SCF-induced ear swelling.
Prevented increases in vascular permeability measured by Evans blue dye extravasation.
Chemical Information
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No. CAS 3080682-14-7
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Peso molecular 376.39
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Fòrmula C20H17FN6O
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SMILES
CC1=C(C=C(C(F)=C1)C2=NN=C(N2)C3CC3)NC(C4=C5C=CC=CN5N=C4)=O
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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.
Protocolo
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Transepithelial/transendothelial electrical resistance assay
TEER measures electrical resistance across epithelial or endothelial monolayers cultured on permeable supports, and the readout reflects ionic conductance through the cell barrier, especially the paracellular pathway regulated by junctional integrity. TEER can be measured without destroying the monolayer and is commonly used before or during transport, permeability, barrier-disruption, and barrier-maturation experiments. TEER values are influenced by biological maturation and technical conditions; reported factors include temperature, medium formulation, passage number, electrode geometry, membrane properties, and junctional length during early monolayer maturation. Therefore, TEER should be interpreted with blank-insert subtraction, area normalization, repeated readings, and, when possible, orthogonal barrier readouts such as FITC-dextran flux or tight-junction staining.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Kit-IN-2 Related Classifications
HY-189056 Related Classifications
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