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.
For research use only. We do not sell to patients.
- Formula: C21H17F2N5O2
- Molecular Weight:409.39
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
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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Molecular Weight 409.39
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Kit-IN-3 Related Classifications
HY-189799 Related Classifications
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