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G5-7

Catalog No. T8742 CAS 939681-36-4

Synonyms: JAK2 inhibitor G5-7

JAK2 inhibitor G5-7 (JAK2 inhibitor G5-7) is an orally active JAK2 inhibitor, selectively inhibits JAK2–mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by binding to JAK2. G5-7 has the potential for glioma study

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G5-7, CAS 939681-36-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 76.00
5 mg	In stock	$ 163.00
10 mg	In stock	$ 247.00
25 mg	In stock	$ 455.00
50 mg	In stock	$ 657.00
100 mg	In stock	$ 918.00
500 mg	In stock	$ 1,830.00
1 mL * 10 mM (in DMSO)	In stock	$ 178.00

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Purity: 99.37%

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Description

In vitro

G5-7 that selectively inhibited Janus kinase 2 (JAK2)-mediated phosphorylation and activation of EGFR and STAT3 (signal transducer and activator of transcription 3) by binding to JAK2, thereby decreasing the activity of downstream signaling by mTOR (mammalian target of rapamycin) and inducing cell cycle arrest.?G5-7 inhibited the proliferation of PTEN-deficient glioblastoma cell lines harboring a constitutively active variant of EGFR (U87MG/EGFRvIII) and human glioblastoma explant neurosphere cultures, but the drug only weakly inhibited the proliferation of either glioblastoma cell lines that were wild type for EGFR and stably transfected with PTEN (U87MG/PTEN) or normal neural progenitor cells and astrocytes.?Additionally, G5-7 reduced vascular endothelial growth factor (VEGF) secretion and endothelial cell migration and induced apoptosis in glioblastoma xenografts, thereby suppressing glioblastoma growth in vivo.?Furthermore, G5-7 was more potent than EGFR or JAK2 inhibitors that interfere with either ligand or adenosine 5'-triphosphate (ATP) binding at impeding glioblastoma cell proliferation.

Synonyms	JAK2 inhibitor G5-7
Molecular Weight	383.39
Formula	C22H19F2NO3
CAS No.	939681-36-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 22.5 mg/mL (58.69 mM)

References and Literature

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

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library Bioactive Compound Library Reprogramming Compound Library Anti-Pancreatic Cancer Compound Library Anti-Cancer Compound Library Apoptosis Compound Library Covalent Inhibitor Library Orally Active Compound Library Kinase Inhibitor Library

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Keywords

G5-7 939681-36-4 Angiogenesis Apoptosis Chromatin/Epigenetic JAK/STAT signaling Stem Cells JAK antiangiogenic inhibit Glioma G-5-7 cycle G5 7 phase G57 STAT3 cell Inhibitor JAK2 inhibitor G5-7 EGFR Janus kinase mTOR inhibitor

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