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] | |
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. |
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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. |
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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 |
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溶解性数据 | In Vitro: DMSO : 83.33 mg/mL(217.35 mM;Need ultrasonic) 配制储备液 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℃, 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。 |