G5-7CS-01Y65811_上海莼试生物技术有限公司

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一、概述：

化学性质：

规格	5 mg 10 mg 25 mg
CAS	939681-36-4
别名	N/A
化学名	N/A
分子式	C22H19F2NO3
分子量	383.39
溶解度	DMSO : 83.33 mg/mL (217.35 mM; Need ultrasonic)
储存条件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

产品描述：

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].

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].

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

[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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标签：G5-7

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