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

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 EGFRSTAT3 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。

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G5-7 Chemical Structure

G5-7 Chemical Structure

CAS No. : 939681-36-4

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1760
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1 mg ¥570
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5 mg ¥1600
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10 mg ¥2500
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25 mg ¥4300
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查看 JAK 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

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.
体内研究
(In Vivo)

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

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.
分子量

383.39

Formula

C22H19F2NO3

CAS 号
性状

固体

颜色

Off-white to light yellow

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 中的溶解度 : 83.33 mg/mL (217.35 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 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
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.

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