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G5-7

SKU: orb1298669

Description

G5-7 is an orally bioavailable, selective JAK2 inhibitor that suppresses JAK2-mediated EGFR (Tyr1068) and STAT3 phosphorylation. It has demonstrated potential for glioma research in both cellular and animal models, showing efficacy in inhibiting tumor growth and related signaling pathways.

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Images & Validation

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G5-7

Key Properties

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CAS Number939681-36-4
MW383.39
Purity99.37% (May vary between batches)
FormulaC22H19F2NO3
SMILESCCOC(=O)N1C\C(=C\c2ccccc2F)C(=O)\C(C1)=C/c1ccccc1F
TargetJAK,Apoptosis
SolubilityDMSO:22.5 mg/mL (58.69 mM)

Bioactivity

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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.
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Storage & Handling

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StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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cycle, Apoptosis, JAK2 inhibitor G5-7, JAK, JAK2, G57, G-5-7, G5-7, G5 7, Glioma, phase, STAT3
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Compound Identifiers

PubChem CID
162640594 ↗

Key Properties

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No computed properties available.

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G5-7 (orb1298669)

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% DMSO +
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% Tween 80 +
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Available Sizes

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1 mg
$ 80.00
5 mg
$ 110.00
1 ml x 10 mM (in DMSO)
$ 120.00
10 mg
$ 150.00
25 mg
$ 240.00
50 mg
$ 320.00
100 mg
$ 430.00
200 mg
$ 570.00
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