2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis
  3. JAK Apoptosis
  4. G5-7

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.

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G5-7 Chemical Structure

G5-7 Chemical Structure

CAS No. : 939681-36-4

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 220 In-stock
Solution
10 mM * 1 mL in DMSO USD 220 In-stock
Solid
1 mg USD 95 In-stock
5 mg USD 200 In-stock
10 mg USD 300 In-stock
25 mg USD 550 In-stock
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Based on 1 publication(s) in Google Scholar

G5-7 Related Antibodies

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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].

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

G5-7 Related Antibodies

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].

MedChemExpress (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.
Appearance

Solid

Color

Off-white to light yellow

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6083 mL 13.0415 mL 26.0831 mL 65.2077 mL
5 mM 0.5217 mL 2.6083 mL 5.2166 mL 13.0415 mL
10 mM 0.2608 mL 1.3042 mL 2.6083 mL 6.5208 mL
15 mM 0.1739 mL 0.8694 mL 1.7389 mL 4.3472 mL
20 mM 0.1304 mL 0.6521 mL 1.3042 mL 3.2604 mL
25 mM 0.1043 mL 0.5217 mL 1.0433 mL 2.6083 mL
30 mM 0.0869 mL 0.4347 mL 0.8694 mL 2.1736 mL
40 mM 0.0652 mL 0.3260 mL 0.6521 mL 1.6302 mL
50 mM 0.0522 mL 0.2608 mL 0.5217 mL 1.3042 mL
60 mM 0.0435 mL 0.2174 mL 0.4347 mL 1.0868 mL
80 mM 0.0326 mL 0.1630 mL 0.3260 mL 0.8151 mL
100 mM 0.0261 mL 0.1304 mL 0.2608 mL 0.6521 mL
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G5-7 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

G5-7939681-36-4JAKApoptosisJanus kinaseEGFRSTAT3GliomaG2phaseantiangiogeniccellcyclemTORInhibitorinhibitorinhibit

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