E7090|cas:1622204-21-0|西域试剂

E7090,99.64%

产品编号：Bellancom-101466| CAS NO：1622204-21-0| 分子式：C₃₂H₃₇N₅O₆| 分子量：587.67

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-101466	￥3200.00	杭州北京（现货）
Bellancom-101466	￥8500.00	杭州北京（现货）
Bellancom-101466	￥14500.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

E7090

产品介绍

E7090 是一种有效的，具有口服活性的选择性 FGFR 抑制剂，对 FGFR1/FGFR2/FGFR3/FGFR4 的 IC₅₀ 值分别为 0.71 nM、0.50 nM、1.2 nM 和120 nM。

生物活性

E7090 is an orally available, potent, and selective FGFR inhibitor with IC₅₀s of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/FGFR2/FGFR3/FGFR4, respectively.

体外研究

E7090 inhibits the growth of SNU-16, human gastric cancer cell line harboring FGFR2 amplification with an IC₅₀ value of 3 nM.
E7090 inhibits SNU-16 cell proliferation with an IC₅₀ value of 5.7 nM.
E7090 inhibits proliferation of human cancer cell lines harboring various types of FGFRs gene abnormalities such as amplification, mutation, or translocation in vitro, which are confirmed by the inhibition of FGFR signaling.
E7090 has interaction kinetics with FGFR1 kinases intermediate between those of the two representative inhibitors, and the residence time of E7090 succinate is 19 minutes.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell Line:	SNU-16 cells
Concentration:	0.4-100 nM
Incubation Time:	4 hours
Result:	Inhibited FGFR phosphorylation with an IC₅₀ value of 1.2 nM. Inhibited the phosphorylation of FRS2a, ERK1/2, and AKT, molecules downstream of FGFRs, in a dose-dependent manner.

体内研究
(In Vivo)

Pharmacodynamics analysis reveals that E7090 inhibits phosphorylation of FGFRs in SNU-16 xenograft tumors in a dose-dependent manner.
E7090 (6.25-50 mg/kg, orally, once daily) treatment prolongs survival in a 4T1 mouse lung metastasis model.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Mouse xenograft model of SNU-16 human gastric cancer
Dosage:	6.25 to 50 mg/kg
Administration:	Orally, once daily for 14 days
Result:	Inhibited tumor growth in a dose-dependent manner.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Mouse xenograft model of SNU-16 human gastric cancer
Dosage:	6.25 to 50 mg/kg
Administration:	Orally, once daily for 14 days
Result:	Inhibited tumor growth in a dose-dependent manner.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Mouse xenograft model of SNU-16 human gastric cancer
Dosage:	6.25 to 50 mg/kg
Administration:	Orally, once daily for 14 days
Result:	Inhibited tumor growth in a dose-dependent manner.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (170.16 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7016 mL	8.5082 mL	17.0164 mL
5 mM	0.3403 mL	1.7016 mL	3.4033 mL
10 mM	0.1702 mL	0.8508 mL	1.7016 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°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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.25 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.25 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.25 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。