G5-7

• CAT Number: I045577
• CAS Number: 939681-36-4
• Molecular Formula: C22H19F2NO3
• Molecular Weight: 383.39
• Purity: ≥95%
• Synonyms: ethyl (3Z,5Z)-3,5-bis[(2-fluorophenyl)methylidene]-4-oxopiperidine-1-carboxylate
• InChI: InChI=1S/C22H19F2NO3/c1-2-28-22(27)25-13-17(11-15-7-3-5-9-19(15)23)21(26)18(14-25)12-16-8-4-6-10-20(16)24/h3-12H,2,13-14H2,1H3/b17-11-,18-12-
• InChIKey: FPAYMMBGZTYNSI-WHYMJUELSA-N
• SMILES: CCOC(=O)N1CC(=CC2=CC=CC=C2F)C(=O)C(=CC3=CC=CC=C3F)C1

G5-7, an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr1068) 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[1].
G5-7 (0-5 μM) inhibits EGFR tyrosine phosphorylation and downstream mTOR signaling and arrests the cell cycle at G2 phase[1].
G5-7 does not directly inhibit EGFR activation[1].
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[1].
G5-7 interacts with full-length JAK2[1].
G5-7 significantly inhibits EGFR Tyr1068 phosphorylation but had no effect on EGFR Tyr1045 phosphorylation[1].
G5-7 downregulates the downstream signaling of JAK by mTOR[1].
G5-7 (10 and 50 mg/kg, oral gavege) decreases VEGF secretion and exerts a potent antiangiogenic effect[1].

Reference

[1]. Kunyan He, et al. Blockade of glioma proliferation through allosteric inhibition of JAK2. Sci Signal. 2013 Jul 9;6(283):ra55.
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