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G5-7, an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr 1068 ) and STAT3 by binding to JAK2 . G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect. G5-7 has the potential for glioma study
In Vitro
G5-7 (0-5 μM) inhibits EGFR tyrosine phosphorylation and downstream mTOR signaling and arrests the cell cycle at G2 phase. G5-7 does not directly inhibit EGFR activation. G5-7 (0-10 μM) comparably increases the abundance of markers (cleved-PARP and caspase 3) of apoptosis in parental LN229 cells and U87MG/EGFRvIII cells. G5-7 interacts with full-length JAK2. G5-7 significantly inhibits EGFR Tyr1068 phosphorylation but had no effect on EGFR Tyr1045 phosphorylation. G5-7 downregulates the downstream signaling of JAK by mTOR. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot Analysis. Cell Line: U87MG/PTEN cells. Concentration: 0-5 μM. Incubation Time: 6 hours. Result: Blocked EGFR phosphorylation and cell cycle at G2 phase to inhibit cell proliferation.
In Vivo
G5-7 (10 and 50 mg/kg, oral gavege) decreases VEGF secretion and exerts a potent antiangiogenic effect . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Cells (4 × 10 6 ) in 100 μl of serum-free DMEM were inoculated subcutaneously into 5- to 6-week-old female nude mice . Dosage: 10 and 50 mg/kg. Administration: Oral gavage. Result: Suppresses angiogenesis in tumors.
Form:Solid
IC50& Target:JAK2
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Consultar COA →Resumo de referência rápida das especificações e aplicações do produto.
Ver ficha técnica →Atributos de qualidade completos e critérios de aceitação para este grau.
Ver folha de especificações →Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organoheterocyclic compounds |
| Classe | Piperidines |
| Subclass | Piperidinecarboxylic acids and derivatives |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Piperidinecarboxylic acids |
| Alternative Parents | Piperidinones Fluorobenzenes Aryl fluorides Carbamate esters Cyclic ketones Azacyclic compounds Organonitrogen compounds Organofluorides Organic oxides Hydrocarbon derivatives |
| Molecular Framework | Aromatic heteromonocyclic compounds |
| Substituents | Piperidinecarboxylic acid - Fluorobenzene - Halobenzene - Piperidinone - Aryl fluoride - Aryl halide - Monocyclic benzene moiety - Benzenoid - Carbamic acid ester - Ketone - Cyclic ketone - Azacycle - Hydrocarbon derivative - Organic oxide - Organooxygen compound - Organonitrogen compound - Organofluoride - Organohalogen compound - Organic oxygen compound - Organic nitrogen compound - Carbonyl group - Aromatic heteromonocyclic compound |
| Descrição | This compound belongs to the class of organic compounds known as piperidinecarboxylic acids. These are compounds containing a piperidine ring which bears a carboxylic acid group. |
| External Descriptors | Not available |
| Solubilidade | DMSO : 83.33 mg/mL (217.35 mM; Need ultrasonic) |
|---|