您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > G5-7
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
G5-7
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
G5-7图片
CAS NO:939681-36-4
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

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 allostericJAK2inhibitor, selectively inhibitsJAK2mediated phosphorylation and activation ofEGFR(Tyr1068) andSTAT3by binding toJAK2. G5-7 induces cell cycle arrest,apoptosisand 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].

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].

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

性状

Solid

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°C3 years
In solvent-80°C6 months
-20°C1 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 mg5 mg10 mg
1 mM2.6083 mL13.0415 mL26.0831 mL
5 mM0.5217 mL2.6083 mL5.2166 mL
10 mM0.2608 mL1.3042 mL2.6083 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。