3080682-21-6
Chemical Structure
Kit-IN-1
- CAS No.: 3080682-21-6
- Formula:C20H16F2N6O
- Molecular Weight:394.38
InChIKey: IBYIEMJBGNBMGU-UHFFFAOYSA-N
SMILES: FC1=CN2N=CC(C(NC3=C(C)C=C(F)C(C4=NN=C(C5CC5)N4)=C3)=O)=C2C=C1
Biological Activity: 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[1].
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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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