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JAK2 inhibitor G5-7

Chemical Structure : JAK2 inhibitor G5-7

CAS No.: 939681-36-4

JAK2 inhibitor G5-7 (G5-7)

Catalog No.: PC-35502Not For Human Use, Lab Use Only.

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.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.
G5-7 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.
G5-7 significantly inhibits EGFR Tyr1068 phosphorylation but has no effect on EGFR Tyr1045 phosphorylation.
G5-7 decreases GBM tumor volume and extends the life span of tumor-bearing nude mice after oral administration.

Physicochemical Properties

M.Wt 383.395
Formula C22H19F2NO3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

1. He K, et al. Sci Signal. 2013 Jul 9;6(283):ra55.

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