GNF-2
≥98% (HPLC), solid
DOWNLOAD MSDS (PDF)Synonym:
3-
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CAS Number 778270-11-4
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Empirical Formula (Hill Notation) C18H13F3N4O2
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Molecular Weight 374.32
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MDL number MFCD09265253
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PubChem Substance ID 24724498
Properties
| Related Categories | Apoptosis Inhibitors, Apoptosis and Cell Cycle, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience, |
| assay | ≥98% (HPLC) |
| form | solid |
| color | off-white |
| solubility | H2O: <2 mg/mL |
| DMSO: ≥5 mg/mL | |
| storage temp. | 2-8°C |
Description
Biochem/physiol Actions
GNF-2 belongs to a new class of Bcr-abl inhibitors. GNF-2 appears to bind to the myristoyl binding pocket, an allosteric site distant from the active site, stabilizing the inactive form of the kinase. It inhibits Bcr-abl phosphorylation with an IC50 of 267 nM, but does not inhibit a panel of 63 other kinases, including native c-Abl, and shows complete lack of toxicity towards cells not expressing Bcr-Abl. GNF-2 shows great potential for a new class of inhibitor to study Bcr-abl activity and to treat resistant Chronic myelogenous leukemia (CML), which is caused the Bcr-Abl oncoprotein.
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