製品番号: 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.

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純度: 98.45%
CAS 番号: 939681-36-4
分子式: C₂₂H₁₉F₂NO₃
分子量:383.39

保管条件:

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

G5-7 構造式

CAS 番号: 939681-36-4

容量

価格（税別）

在庫状況

数量

Sample (0.1mg)

In-stock

(In Japan)

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生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
溶剤 & 溶解度
- 体外
純度とドキュメンテーション
参考文献
Help & FAQs
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

JAK2

JAK アイソフォーム固有の製品をすべて表示 :

体外実験

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.

体内実験

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.

化学情報

CAS 番号 939681-36-4
性状 Solid
分子量 383.39
分子式 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
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

溶剤 & 溶解度

体外:

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.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (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)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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

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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

JAK アイソフォーム固有の製品をすべて表示

生物活性

化学情報

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

G5-7 関連分類

製品番号: HY-115452