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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- CAS No.: 3080682-14-7
- Formule: C20H17FN6O
- Masse moléculaire:376.39
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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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Help & FAQs
Activité biologique
Description
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.
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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CAS No. 3080682-14-7
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Masse moléculaire 376.39
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Formule 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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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)
Kit-IN-2 Related Classifications
HY-189056 Related Classifications
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