1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
    Apoptosis
  2. JAK
    Apoptosis
  3. G5-7

G5-7 

Cat. No.: HY-115452 Purity: 99.84%
Handling Instructions

G5-7, an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by binding to JAK2. G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect. G5-7 has the potential for glioma study.

For research use only. We do not sell to patients.

G5-7 Chemical Structure

G5-7 Chemical Structure

CAS No. : 939681-36-4

Size Price Stock Quantity
5 mg USD 200 In-stock
Estimated Time of Arrival: December 31
10 mg USD 300 In-stock
Estimated Time of Arrival: December 31
25 mg USD 550 In-stock
Estimated Time of Arrival: December 31
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100 mg   Get quote  

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Description

G5-7, an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by binding to JAK2. G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect. G5-7 has the potential for glioma study[1].

IC50 & Target[1]

JAK2

 

In Vitro

G5-7 (0-5 μM) inhibits EGFR tyrosine phosphorylation and downstream mTOR signaling and arrests the cell cycle at G2 phase[1].
G5-7 does not directly inhibit EGFR activation[1].
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[1].
G5-7 interacts with full-length JAK2[1].
G5-7 significantly inhibits EGFR Tyr1068 phosphorylation but had no effect on EGFR Tyr1045 phosphorylation[1].
G5-7 downregulates the downstream signaling of JAK by mTOR[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1].

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.
In Vivo

G5-7 (10 and 50 mg/kg, oral gavege) decreases VEGF secretion and exerts a potent antiangiogenic effect[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Cells (4 × 106) in 100 μl of serum-free DMEM were inoculated subcutaneously into 5- to 6-week-old female nude mice[1].
Dosage: 10 and 50 mg/kg.
Administration: Oral gavage.
Result: Suppresses angiogenesis in tumors.
Molecular Weight

383.39

Formula

C₂₂H₁₉F₂NO₃

CAS No.

939681-36-4

SMILES

O=C(N1C/C(C(/C(C1)=C\C2=CC=CC=C2F)=O)=C/C3=CC=CC=C3F)OCC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 83.33 mg/mL (217.35 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6083 mL 13.0415 mL 26.0831 mL
5 mM 0.5217 mL 2.6083 mL 5.2166 mL
10 mM 0.2608 mL 1.3042 mL 2.6083 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

G5-7JAKApoptosisJanus kinaseEGFRSTAT3GliomaG2phaseantiangiogeniccellcyclemTORInhibitorinhibitorinhibit

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Product Name:
G5-7
Cat. No.:
HY-115452
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