G5-7|cas:939681-36-4|西域试剂

G5-7,99.84%

产品编号：Bellancom-115452| CAS NO：939681-36-4| 分子式：C₂₂H₁₉F₂NO₃| 分子量：383.39

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-115452	￥2000.00	杭州北京（现货）
Bellancom-115452	￥3000.00	杭州北京（现货）
Bellancom-115452	￥5500.00	杭州北京（现货）

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G5-7

产品介绍

G5-7 是具有口服活性的 JAK2 变构抑制剂，可通过结合到 JAK2，选择性的抑制 JAK2 介导的 EGFR 和 STAT3 的磷酸化和激活。G5-7 诱导细胞周阻滞和诱导凋亡、具有抗血管生成活性。G5-7 有用于胶质瘤研究的潜能。

生物活性

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.

体外研究

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

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

Western Blot Analysis.

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.

体内研究
(In Vivo)

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

西域 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.
Dosage:	10 and 50 mg/kg.
Administration:	Oral gavage.
Result:	Suppresses angiogenesis in tumors.

体内研究

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

西域 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.
Dosage:	10 and 50 mg/kg.
Administration:	Oral gavage.
Result:	Suppresses angiogenesis in tumors.

体内研究

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

西域 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.
Dosage:	10 and 50 mg/kg.
Administration:	Oral gavage.
Result:	Suppresses angiogenesis in tumors.

性状

Solid

溶解性数据

In Vitro:

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

配制储备液

浓度溶剂体积质量	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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献

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

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产品编号(Item Number)

批号(Lot Number)

G5-7,99.84%

G5-7

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