G5-7

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

G5-7  纯度: 99.84%

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。

G5-7

G5-7 Chemical Structure

CAS No. : 939681-36-4

规格 价格 是否有货 数量
5 mg ￥2000 In-stock
10 mg ￥3000 In-stock
25 mg ￥5500 In-stock
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100 mg   询价  

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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[1].

IC50 & Target[1]

JAK2

 

体外研究
(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].

上海金畔生物科技有限公司 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.

体内研究
(In Vivo)

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

上海金畔生物科技有限公司 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.

分子量

383.39

Formula

C22H19F2NO3
CAS 号

939681-36-4
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
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。
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.

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