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.
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- 화학식: C21H17F2N5O2
- 분자량:409.39
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
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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분자량 409.39
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화학식 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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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-3 Related Classifications
HY-189799 Related Classifications
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