Kit-IN-1
Kit-IN-1 is a kinome-selective and orally active KIT inhibitor with a human IC50 value of 2.8 nM. Kit-IN-1 binds to KIT in an allosteric mode, stabilizes the inactive DFG-out conformation of KIT, and blocks the stem cell factor (SCF)-mediated KIT phosphorylation signaling pathway. Kit-IN-1 inhibits SCF-induced ear swelling in rats and prevents increased vascular permeability. Kit-IN-1 can be used in studies related to mast cell-driven chronic inflammation.
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- CAS No.: 3080682-21-6
- 화학식: C20H16F2N6O
- 분자량:394.38
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
In Vitro
Kit-IN-1 (compound 7) (0.70 μM; 1-120 min) potently inhibits purified KIT kinase, with an IC50 of 2.8 nM in HTRF assays and 0.89 nM in radiometric assays, and exhibits over 350-fold selectivity over ABL2 kinase[1].
Kit-IN-1 inhibits SCF-induced KIT phosphorylation in M07e cells with an IC50 of 0.16 μM[1].
Kit-IN-1 exhibits excellent selectivity against structurally related kinases, with over 1200-fold selectivity over all type III RTKs (PDGFRα, PDGFRβ, CSF1R, FLT3) and over 610-fold selectivity over DDR1/DDR2; at a concentration of 0.70 μM, its kinome selectivity score S50% is 0.003[1].
Kit-IN-1 exhibits favorable permeability in MDCK-II cells, with moderate efflux mediated by P-gp and BCRP transporters; it also shows good metabolic stability in human and rat hepatocytes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | CL | CLunbound | Vss | MRT | T1/2 | AUC0-∞ | Cmax | Bioavailability |
|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 0.5 mg/kg | i.v. | 0.28 L/h/kg | 15 L/h/kg | 0.91 L/kg | 3.4 h | 2.8 h | / | / | / |
| Mice[1] | 0.5 mg/kg | i.v. | 7.8 L/h/kg | 310 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 | 44 L/h/kg | 0.64 L/kg | 0.81 h | 0.60 h | / | / | / |
| Monkey[1] | 0.5 mg/kg | i.v. | 0.37 L/h/kg | 3.2 L/h/kg | 1.7 L/kg | 4.9 h | 6.1 h | / | / | / |
| Rat[1] | 2.0 mg/kg | p.o. | / | / | / | / | / | 8500 ng/mL | 1200 ng·h/mL | 100 % |
| Dog[1] | 2.0 mg/kg | p.o. | / | / | / | / | / | 2100 ng/mL | 760 ng·h/mL | 76 % |
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 (SD) (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:Significantly reduced SCF-induced ear swelling.
Blocked SCF-induced vascular permeability.
Chemical Information
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CAS No. 3080682-21-6
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분자량 394.38
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화학식 C20H16F2N6O
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SMILES
FC1=CN2N=CC(C(NC3=C(C)C=C(F)C(C4=NN=C(C5CC5)N4)=C3)=O)=C2C=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Kit-IN-1 Related Classifications
HY-187462 Related Classifications
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