Cat. No.: HY-115452

G5-7

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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.

Purity: 98.45%
CAS No.: 939681-36-4
Formula: C₂₂H₁₉F₂NO₃
Molecular Weight:383.39

Storage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

G5-7 Chemical Structure

CAS No.: 939681-36-4

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(In Japan)

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

JAK2

All JAK Isoforms :

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.

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.

Chemical Information

CAS No. 939681-36-4
Appearance Solid
Molecular Weight 383.39
Formula C₂₂H₁₉F₂NO₃
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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Molarity Calculator

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

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

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

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

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G5-7

Apoptosis Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Obesity Compound Library

Anti-Liver Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Cysteine Targeted Covalent Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

All JAK Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

G5-7 Related Classifications

Cat. No.: HY-115452