Description
IC50: 100 nM for FLT3 inhibition SU5614 is a protein tyrosine kinase inhibitor. Tyrosine kinases are enzymes for the activation of many proteins by signal transduction cascades. The proteins are activated by adding a phosphate group to the protein. In vitro: Previous study found that SU5614 could induce growth arrest and apoptosis in c-kit-expressing Kasumi-1, M-07e, and UT-7 cells and inhibited the stem cell factor (SCF)-induced tyrosine phosphorylation of c-kit. Moreover, the sensitivity of Kasumi-1 cells towards the growth inhibitory activity of SU5614 was mainly caused by an autocrine production of SCF, but not by the transforming mutations of c-kit . In vivo: It was found that administration of SU5614, a vascular endothelial growth factor (VEGF) inhibitor, to mice could reduce the levels of VEGF dramatically in BAL fluids 72 h after toluene diisocyanate inhalation. Moreover, consistent with the results obtained from the enzyme immunoassays, Western blot analyses showed that SU5614 reduced the levels of VEGF in the BAL fluid 72 h after toluene diisocyanate inhalation. These results suggested that VEGF might be one of the major determinants of toluene diisocyanate -induced asthma and that the inhibition of VEGF might be a good therapeutic strategy . Clinical trial: Up to now, SU5614 is still in the preclinical development stage.
Product information
CAS Number: 1055412-47-9
Molecular Weight: 272.73
Formula: C15H13ClN2O
Chemical Name: (3Z)-5-chloro-3-[(3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-2,3-dihydro-1H-indol-2-one
Smiles: CC1C=C(C)NC=1/C=C1\C(=O)NC2C=CC(Cl)=CC=2\1
InChiKey: XLBQNZICMYZIQT-GHXNOFRVSA-N
InChi: InChI=1S/C15H13ClN2O/c1-8-5-9(2)17-14(8)7-12-11-6-10(16)3-4-13(11)18-15(12)19/h3-7,17H,1-2H3,(H,18,19)/b12-7-
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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