G5-7

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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。

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°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℃, 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。