JAK2 inhibitor G5-7 chemical structure
Chemical structureResearch use only
CAT. NO. DC11136Featured

JAK2 inhibitor G5-7

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Product overview

Description & Application

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.

ParameterValue
Chemical Nameethyl 3,5-bis((E)-2-fluorobenzylidene)-4-oxopiperidine-1-carboxylate
CAS No.939681-36-4
SynonymsG5-7
FormulaC22H19F2NO3
M.Wt383.395
SMILESN(C(OCC)=O)1C/C(=C\C2=CC=CC=C2F)/C(=O)/C(=C/C2=CC=CC=C2F)/C1
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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; 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.

In Vitro

No in vitro data are provided in the current product source. Contact us for further information.

In Vivo

No in vivo data are provided in the current product source. Contact us for further information.

References & source

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

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

Product documentation

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Handling guide

2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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