JAK2 inhibitor G5-7

Research use only, not for human use.

JAK2 inhibitor G5-7 is a small molecule, allosteric JAK2 inhibitor.

JAK2 inhibitor G5-7 is a small molecule, allosteric JAK2 inhibitor that selectively inhibits JAK2-mediated phosphorylation and activation of EGFR and STAT3 by binding to JAK2; demonstrates inhibitor of U87MG/EGFR and U87MG/EGFRvIII with IC50 of 0.75 and 1.0 uM, arrests cell cycle at G2 phase in both U87MG/EGFRvIII and U87MG/EGFRvIII/PTEN cells; significantly inhibits EGFR Tyr1068 phosphorylation but has no effect on EGFR Tyr1045 phosphorylation; decreases GBM tumor volume and extends the life span of tumor-bearing nude mice after oral administration.

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.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.

G5-7 (10 and 50 mg/kg, oral gavege) decreases VEGF secretion and exerts a potent antiangiogenic effect. Animal Model:Cells (4 × 106) 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.

G5-7

Angiogenesis

JAK

JAK

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939681-36-4

383.395

C22H19F2NO3

>98% (HPLC)

In Vitro:?DMSO : 83.33 mg/mL (217.35 mM)

——

ethyl 3,5-bis((E)-2-fluorobenzylidene)-4-oxopiperidine-1-carboxylate

(-20℃)

With Ice Pack

≥ 2 years